Lach, G., Schellekens, H., Dinan, T. G., & Cryan, J. F.. (2018). Anxiety, Depression, and the Microbiome: A Role for Gut Peptides. Neurotherapeutics
Plain numerical DOI: 10.1007/s13311-017-0585-0
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“The combined methods of analytical thin-layer chromatography (tlc), high-performance tlc, and gas-liquid chromatography (glc) have been used to identify specific alkaloids in twelve cactus species. tlc of fluorescamine conjugates, prepared from primary amines in the alkaloid extracts, served to substantiate results from the other chromatographic identifications. traces of the hallucinogen, mescaline, were identified and quantitated by glc in islaya minor backbg., pereskia corrugata cutak, pereskia tampicana weber, and pereskiopsis scandens br. and r., demonstrating that this alkaloid is distributed through all three cactus tribes.”
McCreary, A. C., Müller, C. P., & Filip, M.. (2015). Psychostimulants: Basic and clinical pharmacology. In International Review of Neurobiology
Plain numerical DOI: 10.1016/bs.irn.2015.02.008
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“Substance use disorder, and particularly psychostimulant use disorder, has considerable socioeconomic burden globally. the psychostimulants include several chemical classes, being derivatives of benzoylecgonine, phenethylamine, phenylpropanolamine, or aminoaryloxazoline. psychostimulant drugs activate the brain reward pathways of the mesoaccumbal system, and continued use leads to persistent neuroplastic and dysfunctional changes of a variety of structures involved in learning and memory, habit-forming learning, salience attribution, and inhibitory control. there are a variety of neurochemical and neurobehavioral changes in psychostimulant addiction, for example, dopaminergic, glutamatergic, serotonergic (5-ht-ergic), and γ-amino butyric acid (gaba) changes have all noted. in this chapter, we will review pharmacological changes associated with psychostimulant use and abuse in humans and animals, and on the basis of the best characterized and most widely abused psychostimulants (amphetamines, cocaine) discuss why use transitions into abuse and review basic science and clinical strategies that might assist in treating psychostimulant abuse.”
Wise, K.. (2016). Response to: “Domestic use of bleach and infections in children: a multicentre cross-sectional study”. Occupational and Environmental Medicine
Plain numerical DOI: 10.1136/oemed-2015-103255
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“The term entheogen is used for psychedelics that are intentionally used spiritually, that is, they generate (engen) the experience of god (theo) within. this chapter offers three big ideas. the first idea is new: we are transitioning from an era of word-based religion to an era of experience-based religion. this change may turn out to be as broad and as deep as the religious transformation 500 years ago when text-based religion replaced the then dominant rite-based religion. the second and third ideas are not new but support the first. the second idea is that mystical experiences form a foundation of religion that gives rise to beliefs, rituals, ethics, and organizations. the third idea is that, under the right conditions, psychedelic plants and chemicals can-but do not always-produce mystical experiences. in this use, they are called entheogens although entheogen use goes back into the mists of archeology (ruck et al. ’2001, rudgley 1993), we are seeing a constant expanding use in the 20th and 21st centuries as the entheogenic path takes its place along with more established paths of transcendence via eclectic types of prayer, meditation, chanting and song, religious services, and other spiritual activities. (psycinfo database record (c) 2016 apa, all rights reserved)”
Mahapatra, A., & Gupta, R.. (2017). Role of psilocybin in the treatment of depression. Therapeutic Advances in Psychopharmacology, 7(1), 54–56.
Plain numerical DOI: 10.1177/2045125316676092
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“Psilocybin is a naturally occurring alkaloid, pharmacologically similar to the classic hallucinogen lysergic acid diethylamide (lsd). although primarily used as a recreational drug or an entheogen in particular cultural settings, recent population based studies have shown that it does not lead to serious physical or mental health problems or dependent use. in view of recent work demonstrating psilocybin’s potential to increase subjective sense of wellbeing and because of its novel mechanism of 5-ht2a serotonin receptor agonism, it is being explored for possible therapeutic utility in mood and anxiety disorders.”
Hansen, M., Phonekeo, K., Paine, J. S., Leth-Petersen, S., Begtrup, M., Bräuner-Osborne, H., & Kristensen, J. L.. (2014). Synthesis and structure-activity relationships of N-benzyl phenethylamines as 5-HT2A/2Cagonists. ACS Chemical Neuroscience
Plain numerical DOI: 10.1021/cn400216u
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“N-benzyl substitution of 5-ht2a receptor agonists of the phenethylamine structural class of psychedelics (such as 4-bromo-2,5-dimethoxyphenethylamine, often referred to as 2c-b) confer a significant increase in binding affinity as well as functional activity of the receptor. we have prepared a series of 48 compounds with structural variations in both the phenethylamine and n-benzyl part of the molecule to determine the effects on receptor binding affinity and functional activity at 5-ht2a and 5-ht2c receptors. the compounds generally had high affinity for the 5-ht2a receptor with 8b having the highest affinity at 0.29 nm but with several other compounds also exhibiting subnanomolar binding affinities. the functional activity of the compounds was distributed over a wider range with 1b being the most potent at 0.074 nm. most of the compounds exhibited low to moderate selectivity (1- to 40-fold) for the 5-ht2a receptor in the binding assays, although one compound 6b showed an impressive 100-fold selectivity for the 5-ht2a receptor. in the functional assay, selectivity was generally higher with 1b being more than 400-fold selective for the 5-ht2a receptor.”
Marek, G. J., & Aghajanian, G. K.. (
1996).
LSD and the phenethylamine hallucinogen DOI are potent partial agonists at 5-HT2A receptors on interneurons in rat piriform cortex.
The Journal of Pharmacology and Experimental Therapeutics
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“Correlations between 5-hydroxytryptamine (5-ht) receptor binding affinities and human hallucinogenic potency have suggested that 5-ht2 receptors mediate the hallucinogenic effects of lysergic acid diethylamide (lsd) and phenethylamine hallucinogens. electrophysiological studies have suggested that a subpopulation of gamma-aminobutyric acid (gaba)ergic interneurons in layer iii of the rat piriform cortex are excited by serotonin (5-ht) via 5-ht2a receptors. these interneurons have inhibitory inputs on pyramidal cells in layer ii. in the present study, we tested low concentrations of both lsd (3-100 nm) and the phenethylamine hallucinogen 1-(2,5-dimethoxy-4-iodophenyl-2-aminopropane (doi; 0.3-10 microm) on rat piriform cortical interneurons that were excited by 5-ht. both lsd (3-100 nm) and doi (0.3-10 microm) excited almost every cell excited by 5-ht. the maximal excitation achieved with lsd and doi was 39% and 55% of the effect of a near-maximal 5-ht concentration (100 microm). consistent with a partial agonist action, lsd and doi blocked the 5-ht excitation of piriform cortical interneurons only at the higher hallucinogen concentrations tested. a specific 5-ht2a receptor antagonist, mdl 100,907, blocked excitation of these interneurons by 5-ht, lsd and doi, but not by norepinephrine or alpha-amino-3-hydroxy-5-methyl-4-isoxazole-propionate. again, consistent with a partial agonist action of the hallucinogens, intracellular experiments showed that a maximal concentration of doi (10 microm) induced fewer postsynaptic inhibitory currents than did 5-ht (100 microm) in pyramidal neurons in layer ii of the piriform cortex. based on the present electrophysiological studies, we conclude that lsd and doi, a phenethylamine hallucinogen, act as highly potent partial agonists at cortical 5-ht2a receptors.”
Arvanov, V. L., Liang, X., Russo, A., & Wang, R. Y.. (1999). LSD and DOB: Interaction with 5-HT2Areceptors to inhibit NMDA receptor-mediated transmission in the rat prefrontal cortex. European Journal of Neuroscience
Plain numerical DOI: 10.1046/j.1460-9568.1999.00726.x
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“Both the phenethylamine hallucinogen (-)-1-2, 5-dimethoxy-4-bromophenyl-2-aminopropane (dob), a selective serotonin 5-ht2a,2c receptor agonist, and the indoleamine hallucinogen d-lysergic acid diethylamide (lsd, which binds to 5-ht1a, 1b, 1d, 1e, 1f, 2a, 2c, 5, 6, 7, dopamine d1 and d2, and alpha1 and alpha2 adrenergic receptors), but not their non-hallucinogenic congeners, inhibited n-methyl-d-aspartate (nmda)-induced inward current and nmda receptor-mediated synaptic responses evoked by electrical stimulation of the forceps minor in pyramidal cells of the prefrontal cortical slices. the inhibitory effect of hallucinogens was mimicked by 5-ht in the presence of selective 5-ht1a and 5-ht3 receptor antagonists. the inhibitory action of dob, lsd and 5-ht on the nmda transmission was blocked by the 5-ht2a receptor antagonists r-(+)-alpha-(2, 3-dimethoxyphenil)-1-[4-fluorophenylethyl]-4-piperidineme thanol (m100907) and ketanserin. however, at low concentrations, when both lsd and dob by themselves only partially depressed the nmda response, they blocked the inhibitory effect of 5-ht, suggesting a partial agonist action. whereas n-(4-aminobutyl)-5-chloro-2-naphthalenesulphonamide (w-7, a calmodulin antagonist) and n-[2-[[[3-(4’-chlorophenyl)- 2-propenyl]methylamino]methyl]phenyl]-n-(2-hydroxyethyl)-4’-methoxy-b enzenesulphonamide phosphate (kn-93, a ca2+/cam-kii inhibitor), but not the negative control 2-[n-4’methoxybenzenesulphonyl]amino-n-(4’-chlorophenyl)-2-propeny l-n -methylbenzylamine phosphate (kn-92), blocked the inhibitory action of lsd and dob, the selective protein kinase c inhibitor chelerythrine was without any effect. we conclude that phenethylamine and indoleamine hallucinogens may exert their hallucinogenic effect by interacting with 5-ht2a receptors via a ca2+/cam-kii-dependent signal transduction pathway as partial agonists and modulating the nmda receptors-mediated sensory, perceptual, affective and cognitive processes.”
Gambelunghe, C., Marsili, R., Aroni, K., Bacci, M., & Rossi, R.. (2013). GC-MS and GC-MS/MS in PCI Mode Determination of Mescaline in Peyote Tea and in Biological Matrices. Journal of Forensic Sciences
Plain numerical DOI: 10.1111/j.1556-4029.2012.02249.x
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“Peyote, a cactus containing the hallucinogen mescaline, is used to induce altered states of consciousness in religious ceremonies or for recreational purpose. this study reports a case of an underage boy suspected of mescaline abuse. for this purpose, we analyzed a dark green liquid sample found in the bedroom of the boy whose urine and hair samples were collected shortly after the drink was found. a method by gas chromatography-mass spectrometry tandem mass spectrometry (gc-ms/ms) in positive chemical ionization mode was developed and validated in terms of linearity, specificity, accuracy, and sensitivity for mescaline determination at the low concentrations present in hair. gc-ms analysis of the liquid identified mescaline, while urine was negative; gc-ms/ms segmental hair analysis identified mescaline in the proximal segment (root to 2 cm), while the distal segments were negative. although peyote was uncommonly encountered, its use was confirmed by segmental hair analysis that can provide long-term information about drugs use.”
Brandt, S. D., Elliott, S. P., Kavanagh, P. V., Dempster, N. M., Meyer, M. R., Maurer, H. H., & Nichols, D. E.. (2015). Analytical characterization of bioactive N-benzyl-substituted phenethylamines and 5-methoxytryptamines. Rapid Communications in Mass Spectrometry
Plain numerical DOI: 10.1002/rcm.7134
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“Advanced glycation end products (ages), s100/calgranulins, hmgb1-proteins, amyloid-beta peptides, and the family of beta-sheet fibrils have been shown to contribute to a number of chronic diseases such as diabetes, amyloidoses, inflammatory conditions, and tumors by promoting cellular dysfunction via binding to cellular surface receptors. the receptor for ages (rage) is a multiligand receptor of the immunoglobulin superfamily of cell surface molecules acting as counter-receptor for these diverse molecules. engagement of rage converts a brief pulse of cellular activation to sustained cellular dysfunction and tissue destruction. the involvement of rage in pathophysiologic processes has been demonstrated in murine models of chronic disease using either a receptor decoy such as soluble rage (srage), rage neutralizing antibodies, or a dominant-negative form of the receptor. studies with rage-/- mice confirmed that rage contributes, at least in part, to the development of late diabetic complications, such as neuropathy and nephropathy, macrovascular disease, and chronic inflammation. furthermore, deletion of rage provided protection from the lethal effects of septic shock caused by cecal ligation and puncture (clp). in contrast, deletion of rage had no effect on the host response in delayed-type hypersensitivity (dth). despite the lack of effect seen in adaptive immunity by the deletion of rage, administration of the receptor decoy, srage, still afforded a protective effect in rage-/- mice. thus, srage is likely to sequester ligands, thereby preventing their interaction with other receptors in addition to rage. these data suggest that, just as rage is a multiligand receptor, its ligands are also likely to recognize several receptors in mediating their biologic effects.”
Braden, M. R., Parrish, J. C., Naylor, J. C., & Nichols, D. E.. (2006). Molecular Interaction of Serotonin 5-HT2A Receptor Residues Phe339(6.51) and Phe340(6.52) with Superpotent N-Benzyl Phenethylamine Agonists. Molecular Pharmacology
Plain numerical DOI: 10.1124/mol.106.028720
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“Experiments were conducted to examine the molecular basis for the high affinity and potency of a new class of 5-ht2a receptor agonists, n-benzyl phenethylamines. competition binding assays at several serotonin receptors confirmed that an n-arylmethyl substitution was necessary for affinity increases up to 300-fold over simple n-alkyl homologs, as well as en- hanced selectivity for 5-ht2a versus 5-ht2c and 5-ht1a recep- tors. pi hydrolysis functional assays confirmed that these n- benzyl phenethylamines are potent and highly efficacious agonists at the rat 5-ht2a receptor. virtual docking of these compounds into a human 5-ht2a receptor homology model indicated that the n-benzyl moiety might be interacting with phe339(6.51) , whereas the phenethylamine portion was likely to be interacting with phe340(6.52) . experiments in h5-ht2a recep- tors with phe339(6.51) l and phe340(6.52) l mutations seem to support support this hypothesis. dramatic detrimental effects on affin- ity, potency, and intrinsic activity were observed with the phe339(6.51) l mutation for all n-benzyl analogs, whereas most n-unsubstituted phenethylamines and traditional agonists were only weakly affected, if at all. consistent with other published studies, the phe340(6.52) l mutation detrimentally affected affin- ity, potency, and intrinsic activity of nearly all compounds tested, although a strong change in intrinsic activity was not seen with most n-aryl analogs. these data further validate the topology of our h5-ht2a receptor homology model. it is note- worthy that this study is the first to identify a hitherto unrecog- nized role for residue 6.51 in agonist activation of a serotonin g protein-coupled receptor (gpcr), whereas most previous re- ports have suggested a varied and sometimes contradictory role in homologous gpcrs.”
Nichols, D. E., Marona-Lewicka, D., Huang, X., & Johnson, M. P.. (
1993).
Novel serotonergic agents.
Drug Des Discov
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“The preliminary structure-activity relationships are described for a series of substituted phenethylamines that induce the release of neuronal serotonin. structures that also have the ability to release neuronal catecholamines are toxic to serotonin neurons, leading to long-term reductions in serotonin markers in rat brain. conversely, compounds that are selective for the serotonin uptake carrier, and do not affect catecholamines, are not neurotoxic. it is suggested that these novel, selective serotonin releasing agents may find therapeutic utility in disorders where serotonin uptake inhibitors are currently employed.”
Ogunbodede, O., McCombs, D., Trout, K., Daley, P., & Terry, M.. (2010). New mescaline concentrations from 14 taxa/cultivars of Echinopsis spp. (Cactaceae) (“ San Pedro” ) and their relevance to shamanic practice. Journal of Ethnopharmacology
Plain numerical DOI: 10.1016/j.jep.2010.07.021
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“Aim of the study: the aim of the present study is to determine in a procedurally uniform manner the mescaline concentrations in stem tissue of 14 taxa/cultivars of the subgenus trichocereus of the genus echinopsis (cactaceae) and to evaluate the relationship (if any) between mescaline concentration and actual shamanic use of these plants. materials and methods: columnar cacti of the genus echinopsis, some of which are used for diagnostic and therapeutic purposes by south american shamans in traditional medicine, were selected for analysis because they were vegetative clones of plants of documented geographic origin and/or because they were known to be used by practitioners of shamanism. mescaline content of the cortical stem chlorenchyma of each cactus was determined by soxhlet extraction with methanol, followed by acid-base extraction with water and dichloromethane, and high-pressure liquid chromatography (hplc). results: by virtue of the consistent analytical procedures used, comparable alkaloid concentrations were obtained that facilitated the ranking of the various selected species and cultivars of echinopsis, all of which exhibited positive mescaline contents. the range of mescaline concentrations across the 14 taxa/cultivars spanned two orders of magnitude, from 0.053% to 4.7% by dry weight. conclusions: the mescaline concentrations reported here largely support the hypothesis that plants with the highest mescaline concentrations – particularly e. pachanoi from peru – are most associated with documented shamanic use. © 2010 elsevier ireland ltd.”
Aghajanian, G. K., & Marek, G. J.. (1999). Serotonin and hallucinogens. Neuropsychopharmacology
Plain numerical DOI: 10.1016/S0893-133X(98)00135-3
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“This brief review traces the serotonin (5-ht) hypothesis of the action of hallucinogenic drugs from the early 1950s to the present day. there is now converging evidence from biochemical, electrophysiological, and behavioral studies that the two major classes of psychedelic hallucinogens, the indoleamines (e.g., lsd) and the phenethylamines (e.g., mescaline), have a common site of action as partial agonists at 5-ht2aand other 5-ht2receptors in the central nervous system. the noradrenergic locus coeruleus and the cerebral cortex are among the regions where hallucinogens have prominent effects through their actions upon a 5-ht2areceptors. recently, we have observed a novel effect ofhallucinogens—a 5-ht2areceptor-mediated enhancement of nonsynchronous, late components of glutamatergic excitatory postsynaptic potentials at apical dendrites of layer v cortical pyramidal cells. we propose that an effect of hallucinogens upon glutamatergic transmission in the cerebral cortex may be responsible for the higher-level cognitive, perceptual, and affective distortions produced by these drugs. © 1999 american college of neuropsychopharmacology.”
Lemaire, D., Jacob, P., & Shulgin, A. T.. (1985). Ring‐substituted β‐methoxyphenethylamines: a new class of psychotomimetic agents active in man. Journal of Pharmacy and Pharmacology
Plain numerical DOI: 10.1111/j.2042-7158.1985.tb03072.x
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“Four members of a new class of psychotomimetic agents have been synthesized and evaluated in man. these compounds, which incorporate a beta-methoxy group onto a beta-phenethylamine sidechain, are the first reported psychotomimetics which are structural analogues of the neurotransmitter noradrenaline. these substances are more potent than the corresponding phenethylamines (lacking a beta-methoxy group) but less potent than the correspondingly substituted amphetamine derivatives.”
Haigler, H. J., & Aghajanian, G. K.. (1973). Mescaline and LSD: Direct and indirect effects on serotonin-containing neurons in brain. European Journal of Pharmacology
Plain numerical DOI: 10.1016/0014-2999(73)90206-9
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“The effects of mescaline and d-lysergic acid diethylamide (lsd) applied by microiontophoresis to single raphe neurons were compared to the effects of mescaline and lsd given systemically. lsd inhibited all raphe cells when given intravenously (i.v.) or microiontophoretically. no decrease in action potential size was seen in either case during the onset or recovery stages. mescaline i.v., 2-8 mg/kg, produced an inhibition of a sub-population of these cells. as in the case of lsd, there was no decrease in action potential size. microiontophoretic mescaline produced a slowing of firing rate at high ejection currents. in contrast to i.v. or microiontophoretic lsd or i.v. mescaline, the slowing produced by microiontophoretic mescaline was always associated with a decrease in action potential size. furthermore, there was no correlation between the populations of cells depressed by microiontophoretic mescaline and i.v. mescaline. these data indicate that mescaline has differing effects on raphe neurons depending on whether it is given systemically or microiontophoretically. in contrast, lsd given systemically or microiontophoretically has similar effects on raphe neurons. © 1973.”
Bullis, R. K.. (2008). The “Vine of the Soul” vs. The Controlled Substances Act: Implications of the Hoasca Case. Journal of Psychoactive Drugs, 40(2), 193–199.
Plain numerical DOI: 10.1080/02791072.2008.10400630
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“In 2006, the supreme court paved the way for the sacramental use of a hallucinogen, hoasca, to be imported, distributed and ingested by a religious group. this case has broad implications for religious freedom for using sacramental psychotropics and how such cases might be decided in the future. this article outlines the arguments used both by the church and by the government. it lists the facts of the cases, explains and analyzes the decision, evaluates the likelihood of expansions of religion-based exceptions for entheogen use in light of the supreme court’s decision and offers a profile for those groups most likely to receive such an exemption. [publication abstract]”
Roberts, T. B.. (
2014).
From the 500-year blizzard of words to personal sacred experiences–The new religious era.. In Seeking the sacred with psychoactive substances: Chemical paths to spirituality and to God: History and practices; Insights, arguments, and controversies, Vols. 1-2.
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“The term entheogen is used for psychedelics that are intentionally used spiritually, that is, they generate (engen) the experience of god (theo) within. this chapter offers three big ideas. the first idea is new: we are transitioning from an era of word-based religion to an era of experience-based religion. this change may turn out to be as broad and as deep as the religious transformation 500 years ago when text-based religion replaced the then dominant rite-based religion. the second and third ideas are not new but support the first. the second idea is that mystical experiences form a foundation of religion that gives rise to beliefs, rituals, ethics, and organizations. the third idea is that, under the right conditions, psychedelic plants and chemicals can—but do not always—produce mystical experiences. in this use, they are called entheogens although entheogen use goes back into the mists of archeology (ruck et al. ‘2001, rudgley 1993), we are seeing a constant expanding use in the 20th and 21st centuries as the entheogenic path takes its place along with more established paths of transcendence via eclectic types of prayer, meditation, chanting and song, religious services, and other spiritual activities. (psycinfo database record (c) 2016 apa, all rights reserved)”
La Barre, W.. (1979). Peyotl and mescaline. Journal of Psychoactive Drugs
Plain numerical DOI: 10.1080/02791072.1979.10472090
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Bruhn, J. G., De Smet, P. A. G. M., El-Seedi, H. R., & Beck, O.. (2002). Mescaline use for 5700 years. The Lancet, 359(9320), 1866.
Plain numerical DOI: 10.1016/S0140-6736(02)08701-9
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“This paper examines urban development in china through the perspective of economic restructuring. first a review of the establishment of an export- oriented economy and its institutional foundation vis-à-vis fiscal and land policies. then an examination of the basic characteristics of the world’s factory model and how it defines the process of urbanization and urban development. comparisons of contrasting spatial forms of upper market commodity housing estates and migrants’ villages point toward a hybrid urban form that essentially reflects the contradiction of the world’s factory regime. finally some specula- tions about the transition of the world’s factory regime and the impact of recent global economic crisis on china’s urban development.”
Bradshaw, C. M., Roberts, M. H. T., & Szabadi, E.. (1971). Effect of mescaline on single cortical neurones. British Journal of Pharmacology
Plain numerical DOI: 10.1111/j.1476-5381.1971.tb07225.x
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“The effects of mescaline upon single cortical neurones were studied, using the microiontophoretic technique. mescaline elicited excitatory and depressant responses similar to those evoked by noradrenaline (na) and 5-hydroxytryptamine (5-hi). the responses to na and mescaline were usually in the same direction, the neurone being either excited by both drugs or depressed by both drugs. the correlation between the effects of mescaline and 5-ht, however, was less consistent. the beta-adrenoceptor blocking agent mj-1999 and the 5-ht antagonist methysergide were both effective in antagonizing mescaline responses.”
Nichols, D. E., Snyder, S. E., Oberlender, R., Johnson, M. P., & Huang, X.. (1991). 2, 3-Dihydrobenzofuran Analogues of Hallucinogenic Phenethylamines. Journal of Medicinal Chemistry
Plain numerical DOI: 10.1021/jm00105a043
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“Two 2,3-dihydrobenzofuran analogues of hallucinogenic amphetamines were prepared and evaluated for activity in the two-lever drug-discrimination paradigm in rats trained to discriminate saline from lsd tartrate (0.08 mg/kg) and for the ability to displace [125i]-(r)-doi [( 125i]-(r)-1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane) from rat cortical homogenate 5-ht2 receptors. the compounds, 1-(5-methoxy-2,3-dihydrobenzofuran-4-yl)-2-aminopropane (6a) and its 7-brominated analogue 6b, possessed activity comparable to their conformationally flexible counterparts 1-(2,5-dimethoxyphenyl)-2-aminopropane (3) and its 4-bromo derivative dob (5), respectively. the results suggest that the dihydrofuran ring in 6a and 6b models the active conformation of the 5-methoxy groups in 3 and 5. free energy of binding, derived from radioligand displacement ka values, indicated that addition of the bromine in either series contributes 2.4-3.2 kcal/mol of binding energy. on the basis of surface area of the bromine atom, this value is 2-3 times higher than would be expected on the basis of hydrophobic binding. thus, hydrophobicity of the para substituent alone cannot account for the dramatic enhancement of hallucinogenic activity. although this substituent may play a minor role in orienting the conformation of the 5-methoxy group in derivatives such as 4 and 5, there appears to be some other, as yet unknown, critical receptor interaction.”
Johnstad, P. G.. (
2018).
Entheogenic Spirituality: Exploring Spirituality Motivated Entheogen Use Among Modern Westerners.
Journal of Ethnographic & Qualitative Research,
12(4),
244–260. Retrieved from http://www.jeqr.org/previous-volumes-1/volume-12-issue-4
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“The use of entheogenic drugs in spiritual contexts among modern west- erners remains an understudied phenomenon. in order to explore these clandestine spiritual practices, 26 anonymous members of an internet discussion fora were interviewed regarding entheogen use and asked to describe their entheogen experiences. interviewees self-selected for par- ticipation, and recruitment was continued until the sample included a diverse range in age, nationality, occupation, and relationship status. respondents were predominantly males with stable jobs and living con- ditions. most participants had extensive entheogen experience. results indicated that respondents tended to follow a pattern of infrequent and often well-planned entheogen use, which they regarded as beneficial to their life and health. entheogen sessions were characterized by insight into self, relations, and world. in addition, participants spoke of inner- visions, feelings of peace, joy, and love, and occasional maslovian peak experiences involving ego dissolution and what they interpreted as contact or unity with transcendent forces. adverse experiences or ‘bad trips’ also occurred, but participants emphasized the long-term value even of these experiences. in general, participants reported long-term consequences of healing and personal growth as the most important reason for entheogen use.”
Kothari, P. J., Hathaway, B. A., Nichols, D. E., & Yim, G. K. W.. (1981). Synthesis and Serotonin-like Activity of 2-Amino-5,8-dimethoxy-6-methyl-l,2-dihydronaphthalene. Journal of Medicinal Chemistry
Plain numerical DOI: 10.1021/jm00139a022
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“As a new type of rigid analogue for hallucinogenic phenethylamines, 2-amino-5,8-dimethoxy-6-methyl-l,2-dihydronaphthalene was synthesized. evaluation in the rat fundus preparation showed it to be a much weaker serotonin agonist than its 1,2,3,4-tetrahydro homologue. both the dihydro and tetrahydro compounds were able to elicit the serotonin syndrome in rats, but with the dihydro compound also appearing weaker in this assay. both rigid analogues were less potent than the known hallucinogen l-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane (dom). © 1981, american chemical society. all rights reserved.”
Barfknecht, C. F., & Nichols, D. E.. (1975). Correlation of psychotomimetic activity of phenethylamines and amphetamines with 1-octanol-water partition coefficients. Journal of Medicinal Chemistry
Plain numerical DOI: 10.1021/jm00236a023
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“In an attempt to relate the hallucinogenic potencies in man of some biologically important amphetamines and phenethylamines, the 1-octanol-water partition coefficients for 11 amphetamines were determined. using these values and published hansch pi constants, the log p for 17 additional amines was estimated. it was found that lipophilicity, as measured by the log of the partition coefficient, may be a significant determinant of the level of hallucinogenic potency. the study also suggests that an ideal log p value for psychotomimetric activity in man may be from 2.89 to 3.72.”
Smith, H.. (2003). Do Drugs have Religious Import?. Psychology, LXI(18), 20.
Plain numerical DOI: 10.2307/2023494
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“Presents an interview with huston smith, one of the most influential scholars of religion of our time, who wrote one of the most influential of all publications on psychedelics in which he took issue with the prevailing view that drugs produced pseudospiritual experiences with little religious value. dr. smith discusses the relationship between psychedelics and the wisdom tradition, the native american church, eleusinian mysteries, and entheogen use. he also talks about how psychedelics have affected his beliefs about death and dying, transmigration of the soul, young people and psychedelics, and the role psychedelics should have in today’s society. (psycinfo database record (c) 2016 apa, all rights reserved)”
Shulgin, A.. (1991). Phenethylamines I Have Known And Loved: A Chemical Love Story. Transform
Plain numerical DOI: 10.1002/jssc.201200424
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“Dispersive liquid-liquid microextraction coupled with high-performance liquid chromatography-ultraviolet detection as a fast and inexpensive technique was applied to the simultaneous extraction and determination of traces of three common herbicides, 2,4-d, alachlor and atrazine, in aqueous samples. the critical experimental parameters, including type of the extraction and disperser solvents as well as their volumes, sample ph, salt addition, extraction time and centrifuging time, and speed were investigated and optimized. under the optimum conditions, the calibration graphs found to be linear in the range of 0.3-200 mug/l with limits of detection in the range of 0.05-0.1 mug/l. the relative standard deviations were in the range of 4.5-6.2% (n = 7). the relative recoveries of well, tap, and river water samples which have been spiked with different levels of herbicides were 92.0-107.0, 82.0-104.0, and 82.0-86.0%, respectively.”
De B. Correia, R., Rust Carmo, L. F., Cecilio, E. L., Bacellar, L. F. H., & Pirmez, L.. (2003). A proactive management and rerouting framework for QoS critical distributed applications using active technology. Proceedings – International Workshop on Object-Oriented Real-Time Dependable Systems, WORDS, 234–241.
Plain numerical DOI: 10.1109/WORDS.2003.1267529
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“Ritual use of peyote among huichols and tarahumara peoples has been documented from the late xxi century onwards. however, the resulting image of these ethnographies seem to lead to irreducible differences. in this article we analyse in a comparative form the relationship between this entheogen, the above mentioned peoples’ worldview, and specifically with the concept of ‘regeneration of life’. it is upon the later that the system of transformations we are presenting in this text roots and articulates itself. (english) [abstract from author]”
Roberts, T. B., & Winkelman, M. J.. (2013). Psychedelic Induced Transpersonal Experiences, Therapies, and Their Implications for Transpersonal Psychology. In The Wiley-Blackwell Handbook of Transpersonal Psychology (pp. 459–479)
Plain numerical DOI: 10.1002/9781118591277.ch25
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“25 psychedelic induced transpersonal experiences, therapies, and their implications for transpersonal psychology thomas b. roberts and michael j.winkelman psychedelics and other natural and synthetic substances have an ability to induce a range of transpersonal experiences. the predominance of spiritually-related experi- ences from these substances has led to the development of the concept of entheogen— reflecting their potential to produce an internal experience of communing with god. the similarity of the drug-induced transpersonal experiences and those induced spon- taneously or through behavioral and mental practices attests to their common bio- logical bases in human nature. these biological bases involve the similarity of these exogenous substances to neurotransmitters, particularly the neuromodulator sero- tonin, and therefore their ability to serve as neurotransmitters. these neurocognitive effects of psychedelics demand a neurophenomenological model that addresses the relationship of both endogenous and exogenous neurotransmitter substances to the nature of perceived reality. these biological foundations also make them important tools for understanding the nature of brain functions, their relationships to mental processes, and the consequential relationship of brain and mind to personal experience, particularly the emotions, health, and spirituality. this chapter presents a neurophe- nomenological model of psychedelic-induced transpersonal experiences, therapeutic processes that they induce, and their implications for transpersonal theory. the phar- macological effects of psychedelics also enables them to address a range of psycho- logical and emotional maladies. the chapter concludes with a brief overview of the multidisciplinary implications of psychedelics for the sciences and society.”
Ruck, C. A. P.. (2014). Entheogens in Ancient Times: Wine and the Rituals of Dionysus. In History of Toxicology and Environmental Health: Toxicology in Antiquity (Vol. 2, pp. 116–125)
Plain numerical DOI: 10.1016/B978-0-12-801506-3.00012-1
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“Entheogen is a neologism used to designate psychoactive substances employed in culturally sanctioned visionary experiences in ritual or religious contexts. the primary divine patron of such experience in classical antiquity was dionysus. his manifestation in the civilized ferment of the grape, which yielded wine, was contrasted with the intoxicants from other sources that preceded viticulture, such as toxic herbs, mushrooms, and animal and insect venoms. emblematic of the contrast was the opposition between the vine and the ivy. the mountain revels of the deity’s female devotees, known as maenads or bacchants, honored the precedents to viticulture in rituals of herb gathering, of which their staff of empowerment, the thyrsus or the narthex, was symbolic. the wine, in contrast, was the drink of the symposium, celebrated by men within the city, with female sexual companions not numbered among the citizenry. the wine itself mediated between the wild and the cultivated in that it was doctored with herbal additives.”
Péri, B.. (2016). “It Is The Weed Of Lovers” The Use Of Cannabis Among Turkic Peoples Up To The 15th Century. Acta Orientalia Academiae Scientiarum Hungaricae, 69(2), 139–155.
Plain numerical DOI: 10.1556/062.2016.69.2.2
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“Cannabis sativa l. is one of the most popular psychoactive plants in our days. it is widely used as a medicine, a recreational drug and also as an entheogen. archaeological findings suggest that the hemp plant was known in china as early as the 5th millennium b.c. the first written source documenting the use of cannabis as a drug is from a much later period and dates back to the 5th century b.c. the present paper offers an outline of the history of the use of cannabis as a mind altering drug among turkic peoples from ancient times up to the late 15th century, a period of flourishing cannabis subculture both in anatolia and in central asia.”
Heiser, M.. (
2017).
PEERANORMAL Episode 07: DMT, Psychedelics, Religious Mysticism, and Paranormal Experiences.
The Naked Bible: Dr. Michael S. Heiser,
2002–2017.
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“This episode focuses on entheogenspsychedelic drugs that are known to cause mystical states of consciousness. our hosts discuss rick strassmans work on dmt, but that is merely a subset of entheogen study. current research in the fields of brain science, psychology, and religion are struggling to explain how entheogens and the experiences they cause should be understood. the dilemma of consciousness, more popularly known as the mind-body problem, is at the heart of the struggle. do entheogens simply affect part of the brain and its chemistry triggering new states of consciousness from inside your head? or do these drugs separate consciousness from the organ of the body we call the brain, verifying that consciousness is distinct from the brain? are god and other supernal beings experienced by people under the effect of entheogens just a product of the brain, or are they entities to be experienced by unhindered consciousness?current research in the fields of brain science, psychology, and religion are struggling to explain how entheogens and the experiences they cause should be understood.”
Rubia Vila, F. J. J.. (
2014).
[Neurospirituality]..
Anales de La Real Academia Nacional de Medicina,
131(1),
307–331. Retrieved from http://pesquisa.bvsalud.org/portal/resource/pt/mdl-27386686
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“Neurospirituality refers to the fact that the brain is able to produce spiritual experiences. the hypothesis put forward here is that the origin of spiritual experiences lies in the hyperactivity of limbic structures within the depth of the temporal lobe. the characteristics of these phenomena are the common denominator of the mystic experiences, the near to death experiences, the symptoms of the temporal lobe epilepsy and those following the consumption of entheogen drugs. experiments with electromagnetic stimulation of the temporal lobe support this hypothesis since they also induce spiritual experiences.”
Fagetti, A.. (
2012).
Cuando “habla” la semilla: adivinación y curación con enteógenos en la Mixteca oaxaqueña. (Spanish).
Revista Cuicuilco
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“The ritual use of the seeds of turbina corymbosa and ipomoea violacea has been documented in colonial historical sources and, in the 20th century, has been recorded and studied in guerrero and oaxaca (mexico). in yodohino and nundó, mixtec villages in the huajuapan de león district, oaxaca, people still use the ‘seeds of the virgin’ (ipomoea violacea) and the seeds of ‘san josé’ (datura stramonium var. godronii) as a means of divination and healing. a woman-expert in the preparation and supply of seeds, which are milled in the ‘metate’ and are mixed with other ingredients-also takes care of the person who drinks the brew, who undergoes a non-ordinary state of consciousness during which ‘the seed speaks’ and reveals what disease afflicts him, why he fell ill and how it can be cured. the article presents the data collected in field on the experience of those who have taken the potion, analyzes the characteristics of the trance and the process during which disease is ‘diagnosed’ and cured; also discuss if this psychoactive potion can be considered an entheogen and if the ritual consumption is part of shamanistic practice. (english) [abstract from author]”
Brown, J. B., & Lupu, M.. (2014). Sacred Plants and the Gnostic Church: Speculations on Entheogen-Use in Early Christian Ritual. Journal of Ancient History, 2(1)
Plain numerical DOI: 10.1515/jah-2014-0010
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“It is the aim of this paper to establish a temporal and cultural link between entheogen-use1 in classical mystery cults and their possible use in a segment of the early christian gnostic church. as early christianity was heavily influenced by the classical world in which it first developed, it is essential to examine the evidence of entheogen-use within classical mystery cults, and explore their possible influence on the development of christian ritual. we will first present textual evidence from the new testament and nag hammadi library (nhl) that indicate possible use of ritual entheogens. next we will examine entheogen-use by some of the main religious sects of the ancient mediterranean world as part of their liturgical practice between c. fifth century bce and the third century ce. then we will show that the different schools of philosophical thought examined were quite fluid, and that there was considerable overlap among schools with respect to several key philosophies and practices. ultimately the subject of entheogen-use in the classical world necessarily falls into the realm of plausible speculation mainly due to the lack of primary sources. however, should the entheogenic hypothesis2 prove to be correct, it promises to be quite useful in future research and in the translation of original documents.”
Monte, A. P., Waldman, S. R., Marona-Lewicka, D., Wainscott, D. B., Nelson, D. L., Sanders-Bush, E., & Nichols, D. E.. (1997). Dihydrobenzofuran analogues of hallucinogens. 4. Mescaline derivatives. Journal of Medicinal Chemistry
Plain numerical DOI: 10.1021/jm970219x
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“Dihydrobenzofuran and tetrahydrobenzodifuran functionalities were employed as conformationally restricted bioisosteres of the aromatic methoxy groups in the prototypical hallucinogen, mescaline (1). thus, 4-(2-aminoethyl)-6,7-dimethoxy-2,3-dihydrobenzofuran hydrochloride (8) and 1-(8-methoxy-2,3,5,6-tetrahydrobenzo[1,2-b:5,4-b’]difuran-4-yl)-2- aminoethane hydrochloride (9) were prepared and evaluated along with 1 for activity in the two-lever drug discrimination (dd) paradigm in rats trained to discriminate saline from lsd tartrate (0.08 mg/kg). also, 1, 8, and 9 were assayed for their ability to displace [3h]ketanserin from rat cortical homogenate 5-ht2a receptors and [3h]8-oh-dpat from rat hippocampal homogenate 5-ht1a receptors. in addition, these compounds were evaluated for their ability to compete for agonist and antagonist binding to cells expressing cloned human 5-ht2a, 5-ht2b, and 5-ht2c receptors. finally, agonist efficacy was assessed by measurement of phosphoinositide hydrolysis in nih 3t3 cells expressing the rat 5-ht2a or 5-ht2c receptors. although 1 fully substituted for lsd in the dd assays (ed50 = 33.5 mumol/kg), neither 8 nor 9 substituted for lsd, with just 50% of the rats administered 8 selecting the drug lever, and only 29% of the rats administered 9 selecting the drug lever. all of the test compounds had micromolar affinity for the 5-ht1a and 5-ht2a receptors in rat brain homogenate. curiously, the rank order of affinities of the compounds at 5-ht2a sites was opposite their order of potency in the behavioral assay. an evaluation for ability to stimulate phosphoinositide turnover as a measure of functional efficacy revealed that all the compounds were of approximately equal efficacy to serotonin in 5-ht2c receptors. at 5-ht2a receptors, however, 8 and 9 were significantly less efficacious, eliciting only 61 and 45%, respectively, of the maximal response. these results are consistent with the proposed mechanism of action for phenethylamine hallucinogens, that such compounds must be full agonists at the 5-ht2a receptor subtype. in contrast to the 2,5-dimethoxy-substituted phenethylamines, where rigidification of the methoxy groups had no deleterious effect on activity, the loss of activity in the 3,4,5-trioxygenated mescaline analogues may suggest that the 3 and 5 methoxy groups must remain conformationally mobile to enable receptor activation.”
Simpson, L., & McKELLAR, P.. (1955). Types of synaesthesia.. The Journal of Mental Science
Plain numerical DOI: 10.1192/bjp.101.422.141
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“Empirical instances of synesthesia from the literature and from the present experiments using mescaline are classified. visual-auditory is the most frequent, but 13 verified types are shown, seven induced by mescaline not occurring with the present subjects. one, algesic-auditory, reported by klüver, is not found in the present series. (psycinfo database record (c) 2010 apa, all rights reserved)”
Ahrendt, K. A., Bergman, R. G., & Ellman, J. A.. (2003). Synthesis of a tricyclic mescaline analogue by catalytic C-H bond activation. Organic Letters
Plain numerical DOI: 10.1021/ol034228d
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“[Reaction: see text] a tetrahydrobis(benzofuran) mescaline analogue has been prepared in six steps and 38% overall yield from (4’-o-methyl)methyl gallate. the key step in this synthesis is a tandem cyclization reaction via directed c[bond]h activation followed by olefin insertion.”
Delbello, M. P., Soutullo, C. A., Hendricks, W., Todd Niemeier, R., McElroy, S. L., & Strakowski, S. M.. (2001). Prior stimulant treatment in adolescents with bipolar disorder: Association with age at onset. Bipolar Disorders, 3(2), 53–57.
Plain numerical DOI: 10.1034/j.1399-5618.2001.030201.x
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“OBJECTIVES: to compare demographic and clinical characteristics between bipolar adolescents with and without a history of stimulant treatment, we hypothesized that adolescents treated with stimulants would have an earlier age at onset of bipolar disorder, independent of co-occurring attention-deficit-hyperactivity disorder (adhd). method: thirty-four adolescents hospitalized with mania were assessed using the washington university at st louis kiddie schedule for affective disorders and schizophrenia (wash-u-ksads). we systematically evaluated age at onset of bipolar disorder and pharmacological treatment history. results: bipolar adolescents with a history of stimulant exposure prior to the onset of bipolar disorder had an earlier age at onset of bipolar disorder than those without prior stimulant exposure. additionally, bipolar adolescents treated with at least two stimulant medications had a younger age at onset compared with those who were treated with one stimulant. there was no difference in age at onset of bipolar disorder between bipolar adolescents with and without adhd. conclusions: our results suggest that stimulant treatment, independent of adhd, is associated with younger age at onset of bipolar disorder. a behavioral sensitization model is proposed to explain our findings. there are several limitations to our study including the small sample size, the retrospective assessment of stimulant exposure and age at onset of bipolar disorder, and the inclusion of only hospitalized patients, who may be more likely to present with a severe illness. nonetheless, future prospective longitudinal investigations that systematically assess the effects of stimulant medications in children with or at genetic risk for bipolar disorder are warranted.”
Arnold, T. C., Hindman, B. W., Walker, A. L., & Ryan, M. L.. (
2005).
Death from ingestion of 2C-T-21: a novel phenethylamine .
Clinical Toxicology
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“Introduction: ‘“2c-t-21,”’ 2,5-dimethoxy-4-(2-fluoroethylthio)phenethylamine, was the last of the 2c-t line of phenethylamines synthesized by alexander shulgin. several favorable ‘“trip reports”’ available via internet regarding this compound and multiple internet sources for purchase have combined to produce this inevitable result. we report a human death. background: from ingestion of 2c-t-21 purchased from an internet source. case report: a 22 year-old male patient presented to his local ed with initial complaints of blurred vision almost immediately after the witnessed ingestion of a small amount of ‘ “2c-t-21”’ which he had recently purchased over the internet from a chemical supply company. later investigation revealed that one-third to three-fourths of the contents from a vial originally containing 1000 mg had been ingested. initial vital signs revealed tachycardia at 132, bp 166/79, temperature 102.2�f, and o2 saturation of 98%. the patients past medical history was significant for being quadriplegic from a motor vehicle collision one year earlier and he was currently being treated for a bladder infection. his current medications included neurontin, tizanidine, prevacid, melatonin, paroxetine and oxybutynin. information was forwarded to the ed regarding management with benzodiazepines and cooling. he quickly developed frank hallucinations, seizures and hyperthermia to 108�f. his pupils became fixed and dilated shortly thereafter. a ct scan performed the next day revealed cerebral edema and hemorrhage. brain death was confirmed on hospital day two. case discussion: to date, this case represents only the second reported death from this compound. although not currently a scheduled substance, cases involving 2c-t-21 have been prosecuted under the federal analogue act. although shulgin has reportedly discontinued his investigation and experimentation with this line of phenethylamines, many others chemistry enthusiasts and opportunists now have the recipe for this dangerous compound. conclusion: we report a case of human death from ingestion of 2c-t-21, a novel psychoactive phenethylamine compound � originally published by taylor & francis in clinical toxicology ”
Klein, M. T., Kalam, M., Street, W., & Terry, M.. (2015). Mescaline concentrations in three principal tissues of Lophophora williamsii (Cactaceae): implications for sustainable harvesting practices. Haseltonia
Plain numerical DOI: 10.2985/026.020.0107
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“We evaluated the pharmacological consequences of tissues other than crown being included with harvested peyote. mean mescaline concentrations were determined for crown, non-chlorophyllous stem, and root, using mature individuals from the same population in south texas. samples of each tissue – crown, non-chlorophyllous stem, and root – were taken from each of 13 individual plants. samples were dried, triturated, defatted, and extracted with methylene chloride, using an acid-base aqueous wash to recover the alkaloids. the concentration of mescaline in each sample was determined by hplc. the average mescaline concentration in non-chlorophyllous stem was an order of magnitude lower than that in crown, whereas the mescaline concentration in root was two orders of magnitude lower than that in crown. these results show that non-chlorophyllous stem is a poor source of mescaline, and root is an extremely poor source. these results have important implications for conservation, suggesting that non-traditional harvesting of peyote for religious or medicinal use involving the cutting of non-chlorophyllous tissue are contributing to the death of plants and the subsequent failure to regenerate new crowns. therefore, this practice should be reevaluated by peyote harvesters and users.”
Páleníček, T., Balíková, M., Bubeníková-Valešová, V., & Horáček, J.. (2008). Mescaline effects on rat behavior and its time profile in serum and brain tissue after a single subcutaneous dose. Psychopharmacology
Plain numerical DOI: 10.1007/s00213-007-0926-5
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“RATIONALE: mescaline is a nonselective serotonin receptor agonist. it has relatively delayed onset of action and prolonged duration. mescaline attenuates various behavioral parameters in rats; however, no information is available about its pharmacokinetics in rats and its relation to the behavioral changes produced by the drug. objectives: the present study evaluates the spontaneous locomotor activity and sensorimotor gating in relation to mescaline concentrations in the serum and the brain of rats materials and methods: behavioral changes induced by mescaline [10, 20, and 100 mg/kg subcutaneously (s.c.)] were evaluated in an open-field test and testing of the prepulse inhibition of acoustic startle reaction (ppi) 15 and 60 min after drug administration. the time disposition of mescaline 20 mg/kg s.c. in rat serum and brain homogenates was analyzed by gas chromatography-mass spectrometry. results: mescaline produced significant inhibitory effects on locomotion in low doses and a biphasic effect with the highest dose. in the ppi test, only when tested 60 min after drug administration, all doses of mescaline disrupted ppi. besides the experimental protocol, we have observed that approximately 50% of animals receiving 100 mg/kg died within 12 h post-injection. the serum levels of mescaline rapidly increased within 30 min and subsequently quickly decreased; however, the brain concentrations reached a maximum 1 h after administration and remained high for an additional 60 min. conclusions: mescaline had a delayed onset of the main behavioral changes in rats compared to other hallucinogens. behavioral changes correlated with the pharmacokinetics of the drug.”
Nagai, F., Nonaka, R., & Satoh Hisashi Kamimura, K.. (2007). The effects of non-medically used psychoactive drugs on monoamine neurotransmission in rat brain. European Journal of Pharmacology
Plain numerical DOI: 10.1016/j.ejphar.2006.11.075
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“We developed a reproducible, simple, and small-scale method for determining the re-uptake and release of monoamines (dopamine, serotonin (5-ht) and norepinephrine) using rat brain synaptosomes. these assays were then applied to study the effects of different kinds of non-medically used psychoactive drugs on monoamine re-uptake and release. the phenethylamine derivatives, 4-fluoroamphetamine, 2-methylamino-3,4-methylene-dioxy-propiophenone (methylone), 1-(1,3-benzodioxol-5-yl)-2-butanamine (bdb), and n-methyl-1-(1,3-benzodioxol-5-yl)-2-butanamine (mbdb), had strong inhibitory effects on the re-uptake of dopamine, 5-ht and norepinephrine. 4-fluoroamphetamine, methylone and bdb also strongly increased the release of the three monoamines, but mbdb increased 5-ht and norepinephrine release, but had little effect on dopamine release. however, 2,5-dimethoxy-4-iodophenethylamine (2c-i), 2,5-dimethoxy-4-ethylphenethylamine (2c-e), 2,5-dimethoxy-4-chlorophenethylamine (2c-c), 2,4,5-trimethoxyamphetamine (tma-2) and 2,4,6-trimethoxyamphetamine (tma-6), which are methoxylated phenethylamine derivatives, slightly influenced the re-uptake and release of monoamines. α-metyltryptamine (amt), a tryptamine derivative, was one of the strongest re-uptake inhibitors and releasers of the three monoamines. the tryptamine derivative, 5-methoxy-α-methyltryptamine (5-meo-amt), also strongly inhibited re-uptake and increased the release of the three monoamines. n,n-dipropyltryptamine (dpt), 5-methoxy-n,n-diisopropyltryptamine (5-meo-dipt), 5-methoxy-n,n-methylisopropyltryptamine (5-meo-mipt), and 5-methoxy-n,n-dimethyltryptamine (5-meo-dmt) inhibited monoamine re-uptake, but had a few effects on monoamine release. 1-(3-chlorophenyl)piperazine (3cpp) and 1-(methoxyphenyl)piperazine (4mpp), which are piperazine derivatives, inhibited monoamine re-uptake and accelerated their release. the results suggest that some designer drugs strongly act on the central nerve system to the same extent as restricted drugs. © 2006 elsevier b.v. all rights reserved.”
Nichols, D. E.. (2012). Structure-activity relationships of serotonin 5-HT2A agonists. Wiley Interdisciplinary Reviews: Membrane Transport and Signaling
Plain numerical DOI: 10.1002/wmts.42
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“Of the 14 known types of serotonin receptors one of the most extensively studied is the 5-ht2a (5-hydroxytryptamine) receptor. in the brain, this receptor plays a key role in regulation of cortical function and cognition, appears to be the principal target for the hallucinogenic/psychedelic drugs such as lysergic acid diethylamide (lsd), and also is a target for the newest atypical antipsychotic agents, which are antagonists or inverse agonists at this site. among the structure–activity relationships that are known for this receptor type, there are three chemical classes of agonists: tryptamines, ergolines, and phenethylamines. important structural features are identified for agonist activity and some of these agonists have features in common. in addition to effects at the receptor will be the focus, these drugs are also hallucinogenic (psychedelic) agents, and much of the sar was developed on the basis of effects in humans, before modern pharmacological techniques were available. a certain amount of our knowledge therefore relies on those human studies. wires membr transp signal 2012, 1:559–579. doi: 10.1002/wmts.42for further resources related to this article, please visit the wires website.”
Glockner, J.. (
2012).
Aquí , allá y en todas partes : trascendencia e inmanencia en el uso de enteógenos.
Cuicuilco
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“The discovery of xochipilli’s sculpture in tlalmanalco and the meeting of gordon wasson with maria sabina in huautla de jimenez in the mid-twentieth century reveal us the millenary ritual history of a gender of psychoactive fungi classified as psilocybe by the modern ethnobotany. from the diffusion in the mass media of wasson and his family’s experience, two social phenomena began to develop: on one hand, the massive consumption of this entheogen by young people traveling to the sierra mazateca compelled by simple curiosity or in search of a mystical experience; and by the other hand, the ingestion by some researchers, writers and intellectuals for different purposes, scientific or philosophical, who have communicated this experience trough their work. the article approaches to some of the most relevant aspects of the ritual as an experience of the transcendent and, at the same time, tries to establish some differences and analogies with the experimental practice as an experience of the immanent. (english) [abstract from author]”
Roberts, T. B., & Hruby, P. J.. (2002). Toward an entheogen research agenda. Journal of Humanistic Psychology, 42(1), 71–89.
Plain numerical DOI: 10.1177/0022167802421004
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“The word entheogen was coined to denote psychedelic chemicals and botanicals that engender the experience of god within. drawing on william james, charles tart, and ken wilber, the authors claim that a complete study of religion must include entheogens, and they propose topics leading toward an entheogen research agenda:(a) the spiritual nature of the human mind, (b) the dispute over the authenticity of entheogen-assisted religious experiences, (c) pastoral counseling, (d) experimental mysticism, (e) entheogenic origins of religion, and (f) policy issues in freedom of conscience and freedom of religion. the authors conclude with seven recommendations to churches, religious orders, seminaries, and scholarly and scientific professional groups for actions they can take to promote entheogenic research.”
Johnstad, P. G.. (2018). Powerful substances in tiny amounts: An interview study of psychedelic microdosing. NAD Nordic Studies on Alcohol and Drugs, 35(1), 39–51.
Plain numerical DOI: 10.1177/1455072517753339
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“Aims:this article presents a qualitative interview study of people who microdose with psychedelic drugs, which means that the user takes about one tenth of an ordinary recreational dose.design:respondents (n = 21) were recruited at several internet fora for individual interviews via private messaging. every participant was male, and the median respondent was in his 30s with a stable job and relationship and extensive entheogen experience.results:respondents tended to experiment with microdosing in phases, reporting mostly positive consequences from this form of drug use. reported effects included improved mood, cognition, and creativity, which often served to counteract symptoms especially from conditions of anxiety and depression. there were also reports of various challenges with psychedelic microdosing, and some did not find the practice worth continuing.conclusion:the study obtained evidence of a group of users taking small doses of psychedelics not for the purpose of intoxication but to enhance every…”
Shulgin, A. T.. (1979). Chemistry of phenethylamines related to mescaline. Journal of Psychoactive Drugs
Plain numerical DOI: 10.1080/02791072.1979.10472091
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“T h is revi ew w ill bri n g toge t h e r a num b e r of the kn own fa cts relat ed t o t he cact us orig ins of t he phcne t hyl a rnin c a lk a lo id s , a c omparison of th eir c h e m ic a l st r u c t ur e s, a list in g o f seve ra l sy nt hetic va r ia nts t ha t a rc kn own a n d a d e script ion of th e psy ch oph arm a-col o gic in to xi cat ion t hat fo llo ws t hei r a d m in ist ra t io n to n or m a l h uma n s u bj e c t s. this w ill be ce nte re d up on t he dr ug m es calin e whi ch is th e m aj or a c ti ve a lk a loi d of thc no rt h am eri c an dumpl in g c a c t u s , kn own b y the common name pey ot e . any one fa milia r w ith the m y s t e ries of tax o n om ic bin om ial n omen cl atur e mu s t be a wa re o f t he co n f us ion a n d fre q u e n t ly p er sona l a rg u me nts th at see m alwa y s to b e underwa y a mo n gst botanist s. t he a r ea o f pe y ote a ss ign m e n t is n o ex c ep t ion . the pe y o t e bu tt on , whi ch is ac ce p t e d as b e in g th e m aj or hallu c ino gen ic cact us in t h is arca , a p pea rs to o c cur in t w o var ia ti ons . bo th co nta in so m e o ne to tw o perc ent a lk a lo id s , but t h ey di ff er in t he co m p o s it io n of th is fr a cti on . in o n e , m esc alin e is t h e m aj or c o m po ne nt ac co m pa n ie d b y s o m e 6 0 o t her a lk a lo ids in les se r a m o u nt s , m o st of t h e m t e t ra hy d ro -iso q u in o li nes . in th e ot her, t h e a lk a lo ids arc lar gel y ph en o li c in na t ure a n d p cll o tin e co n st it u tes a p pro x i-m at e ly 90 p er cent o f thi s fr a cti on . mescalin e is p resent in t racc a mo u nt s a t m o st. t h us wh en th e b u t ton s a rc co lle cte d a t ra n d o m, it is qu it e rea so na b le t hat t he re sho u ld b e w id e va r ia t io n s in co m posit io n rep o rt e d . he ff t er , in h is se m in a l s t u d ies o f va r io us h a t ch es o f pe y ote bu tt on s , e m p lo ye d t he te rms ‘ m esca lin o ge n ic’ *] ·hl3 shu lgin ro ad , l.a fa yer t c. cal iforn ia 9 4 549 . j o urual oj’ l’syc lj/’d elic drugs 4-1 a n d “ pcllot inogc ni c “ to d is t in g u is h t hese t wo ty p es o n a c he m ica l b a si s, but he cl a im ed t hat t h ere wa s n o morph ol ogi cal d ist in ct io n betwee n th em . th ere is , h owe ver , a d istin ct mo r p h o logi ca l vari ant c a lle d i.opbo p b o r« d ilj ilsa w h ic h a p p ea rs to co n tai n la rgely pe llo t ine . wit h a po logi es to t he m o rph ol og ist s a …”
Wolbach, A. B., Miner, E. J., & Isbell, H.. (1962). Comparison of psilocin with psilocybin, mescaline and LSD-25. Psychopharmacologia
Plain numerical DOI: 10.1007/BF00412109
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“Reactions induced by lsd, mescaline, psilocin, and psilocybin are qualitatively similar. the time course of the psilocin and psilocybin reactions are shorter than those of lsd or mescaline reactions. li psilocin is approximately 1.4 times as potent as psilocybin. this ratio is the same as that of the molecular weights of the two drugs”
Rosa, W. E., Hope, S., & Matzo, M.. (2018). Palliative Nursing and Sacred Medicine: A Holistic Stance on Entheogens, Healing, and Spiritual Care. Journal of Holistic Nursing
Plain numerical DOI: 10.1177/0898010118770302
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“The fields of palliative and holistic nursing both maintain a commitment to the care of the whole person, including a focus on spiritual care. advanced serious illness may pose a plethora of challenges to patients seeking to create meaning and purpose in their lives. the purpose of this article is to introduce scholarly dialogue on the integration of entheogens, medicines that engender an experience of the sacred, into the spiritual and holistic care of patients experiencing advanced serious illness. a brief history of the global use of entheogens as well as a case study are provided. clinical trials show impressive preliminary findings regarding the healing potential of these medicinal agents. while other professions, such as psychology, pharmacy, and medicine, are disseminating data related to patient outcomes secondary to entheogen administration, the nursing literature has not been involved in raising awareness of such advancements. research is illustrating their effectiveness in achieving integrative experiences for patients confronting advanced serious illness and their ability to promote presence, introspection, decreased fear, and increased joy and acceptance. evidence-based knowledge surrounding this potentially sensitive topic is necessary to invite understanding, promote scientific knowledge development, and create healing environments for patients, nurses, and researchers alike.”
Blainey, M. G.. (2015). Forbidden Therapies: Santo Daime, Ayahuasca, and the Prohibition of Entheogens in Western Society. Journal of Religion and Health, 54(1), 287–302.
Plain numerical DOI: 10.1007/s10943-014-9826-2
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“Santo daime, a brazilian religion organized around a potent psychoactive beverage called ayahuasca, is now being practiced across europe and north america. deeming ayahuasca a dangerous ‘hallucinogen,’ most western governments prosecute people who participate in santo daime. on the contrary, members of santo daime (called ‘daimistas’) consider ayahuasca a medicinal sacrament (or ‘entheogen’). empirical studies corroborate daimistas’ claim that entheogens are benign and can be beneficial when employed in controlled contexts. following from anthropology’s goal of rendering different cultural logics as mutually explicable, this article intercedes in a misunderstanding between policies of prohibition and an emergent subculture of entheogenic therapy.”
Roberts, T. B.. (
2016).
The entheogen reformation.
Journal of Transpersonal Psychology,
48(1),
26–33.
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“In addition to promising leads for treating ptsd, addictions, depression, and death anxiety, 21st century research at medical schools finds that with careful screening, insightful attention to the variables of set, setting, and dosage, psychedelic drug administration often facilitates significant spiritual experiences, meaningfulness, altruism, well-being, and similar pro- spiritual effects. this article calls for theologians, professors of religious studies, philosophy, sociology, and psychology to update their courses. it challenges leaders of religious organizations, ‘‘how can your institution incorporate these practices and benefit from them?’”
Pickard, L.. (
2008).
The entheogen review.
The Entheogen Review,
XVI(1)
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: “: [Gamma]’ fibrinogen is an isoform of fibrinogen that normally constitutes about 7% of total plasma fibrinogen, and arises from an alternative processing event in the [gamma] chain mrna. [gamma]’ fibrinogen is a newly-emerging cardiovascular disease (cvd) risk factor that appears to have an independent association with cvd from that of total fibrinogen, which is itself a well-established cvd risk factor. [gamma]’ fibrinogen shows a significant association with coronary artery disease and myocardial infarction in at least four case-control studies, including the stockholm coronary artery risk factor study and the framingham heart study. [gamma]’ fibrinogen is also significantly associated with stroke, as shown in the erasmus stroke study and others. the role of genetic polymorphisms in the association between [gamma]’ fibrinogen and cvd is under active investigation, [gamma]’ fibrinogen increases during inflammation, and is differentially regulated from total fibrinogen under pathologic conditions, as demonstrated in the periodontitis and vascular events study. the association between [gamma]’ fibrinogen and venous thromboembolism remains unclear, however, with some studies showing an inverse association with [gamma]’ fibrinogen levels and other studies showing the opposite., copyright (c) 2012 walter de gruyter”
Nichols, D. E., Schooler, D., Yeung, M. C., Oberlender, R. A., & Zabik, J. E.. (1984). Unreliability of the rat stomach fundus as a predictor of hallucinogenic activity in substituted phenethylamines. Life Sciences
Plain numerical DOI: 10.1016/0024-3205(84)90390-4
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“A series of three isomeric 2,4,5-substituted monoethoxy dimethoxy phenylisopropylamines were compared for their contractile effect in the rat fundus and as potential antagonists to the effect of serotonin in the fundus. the three isomers were also evaluated for their discriminative stimulus properties in rats that had been trained to discriminate injections of saline from lsd tartrate (0.08 mg/kg). the drug discrimination studies revealed that the 2,5-dimethoxy-4-ethoxy substitution was most potent in rats, consistent with the reported clinical activity of this isomer in man. by contrast, of the three isomers examined, this was the weakest in eliciting a contraction in the fundus. none of the compounds antagonized serotonin induced contractions, and it was not possible to determine pa2values. questions are raised about the determination of pa2values for partial agonists and it is concluded that the fundus is not a reliable model for prediction of hallucinogenic activity of phenethylamines. © 1984.”
Das, S., Barnwal, P., Ramasamy, A., Sen, S., & Mondal, S.. (2016). Lysergic acid diethylamide: a drug of ‘use’?. Therapeutic Advances in Psychopharmacology, 6(3), 214–228.
Plain numerical DOI: 10.1177/2045125316640440
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“Lysergic acid diethylamide (lsd), described as a classical hallucinogen, began its journey from the middle of the last century following an accidental discovery. since then, it was used as a popular and notorious substance of abuse in various parts of the world. its beneficial role as an adjunct to psychotherapy was much unknown, until some ‘benevolent’ experiments were carried out over time to explore some of its potential uses. but, many of its effects were unclear and seemed to be a psychedelic enigma. in this review article, we have described the receptor pharmacology, mechanism of action, effects and adverse effects of lsd on the normal body system. we have also highlighted its addictive potentials and the chances of developing tolerance. we have assimilated some of the interesting therapeutic uses of this drug, such as an antianxiety agent, a creativity enhancer, a suggestibility enhancer, and a performance enhancer. we have also described lsd to be successfully used in drug and alcohol dependence, and as a part of psychedelic peak therapy in terminally ill patients. the relevant chronological history and literature in the light of present knowledge and scenarios have been discussed. based on available evidence, lsd could be tried therapeutically in certain specific conditions under controlled settings. but as we mention, due to all the safety concerns, the use of this nonaddictive ‘entheogen’ in actual practice warrants a lot of expertise, caution, cooperation and ethical considerations.”
Serra, V., Fattore, L., Scherma, M., Collu, R., Spano, M. S., Fratta, W., & Fadda, P.. (2015). Behavioural and neurochemical assessment of salvinorin a abuse potential in the rat. Psychopharmacology, 232(1), 91–100.
Plain numerical DOI: 10.1007/s00213-014-3641-z
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“RATIONALE: salvinorin a is a recreational drug derived from salvia divinorum, a sage species long used as an entheogen. while salvinorin a has potent hallucinogenic properties, its abuse potential has not been assessed consistently in controlled behavioural and neurochemical studies in rodents. objective: this study aimed to assess salvinorin a abuse potential by measuring its capacity to establish and maintain self-administration behaviour and to modify dopamine (da) levels in the nucleus accumbens (nacc) of rats. results: male lister hooded (lh) and sprague-dawley (sd) rats were allowed to self-administer salvinorin a (0.5 or 1.0 mug/kg/infusion) intravenously 2 h/day for 20 days under a continuous schedule of reinforcement and lever pressing as operandum. lh rats discriminated between the active and inactive levers but did not reach the acquisition criterion for stable self-administration (>/=12 active responses vs /=40 mug/kg) and sd rats (at >/=5 mug/kg), but injection into the ventral tegmental area (vta) induced no significant change in nacc da concentration in lh rats and only brief elevations in sd rats. conclusions: salvinorin a differs from other commonly abused compounds since although it affects accumbal dopamine transmission, yet it is unable, at least at the tested doses, to sustain stable intravenous self-administration behaviour.”
Marek, G. J., & Aghajanian, G. K.. (1998). Indoleamine and the phenethylamine hallucinogens: Mechanisms of psychotomimetic action. Drug and Alcohol Dependence
Plain numerical DOI: 10.1016/S0376-8716(98)00076-3
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“Considers evidence suggesting that both indoleamine and phenethylamine hallucinogens bind to a common neurotransmitter receptor in the brain, the 5-hydroxytryptamine (5-ht) type 2a receptor, and that subsequent activation of this serotonin receptor mediates the psychotomimetic effects of these hallucinogens. the authors also discuss potential site(s) in the brain at which the hallucinogens exert their psychotomimetic effects. (psycinfo database record (c) 2009 apa, all rights reserved)”
McLean, T. H., Chambers, J. J., Parrish, J. C., Braden, M. R., Marona-Lewicka, D., Kurrasch-Orbaugh, D., & Nichols, D. E.. (2006). C-(4,5,6-trimethoxyindan-1-yl)methanamine: A mescaline analogue designed using a homology model of the 5-HT2Areceptor. Journal of Medicinal Chemistry
Plain numerical DOI: 10.1021/jm060272y
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“A conformationally restricted analogue of mescaline, c-(4,5,6-trimethoxyindan-1-yl)-methanamine, was designed using a 5-ht(2a) receptor homology model. the compound possessed 3-fold higher affinity and potency than and efficacy equal to that of mescaline at the 5-ht(2a) receptor. the new analogue substituted fully for lsd in drug discrimination studies and was 5-fold more potent than mescaline. resolution of this analogue into its enantiomers corroborated the docking experiments, showing the r-(+) isomer to have higher affinity and potency and to have efficacy similar to that of mescaline at the 5-ht(2a) receptor.”
Halberstadt, A. L.. (2015). Recent advances in the neuropsychopharmacology of serotonergic hallucinogens. Behavioural Brain Research
Plain numerical DOI: 10.1016/j.bbr.2014.07.016
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“Serotonergic hallucinogens, such as (+)-lysergic acid diethylamide, psilocybin, and mescaline, are somewhat enigmatic substances. although these drugs are derived from multiple chemical families, they all produce remarkably similar effects in animals and humans, and they show cross-tolerance. this article reviews the evidence demonstrating the serotonin 5-ht2areceptor is the primary site of hallucinogen action. the 5-ht2areceptor is responsible for mediating the effects of hallucinogens in human subjects, as well as in animal behavioral paradigms such as drug discrimination, head twitch response, prepulse inhibition of startle, exploratory behavior, and interval timing. many recent clinical trials have yielded important new findings regarding the psychopharmacology of these substances. furthermore, the use of modern imaging and electrophysiological techniques is beginning to help unravel how hallucinogens work in the brain. evidence is also emerging that hallucinogens may possess therapeutic efficacy.”
Richards, W. A.. (2008). The phenomenology and potential religious import of states of consciousness facilitated by psilocybin. In Archive for the Psychology of Religion (Vol. 30, pp. 189–199)
Plain numerical DOI: 10.1163/157361208X317196
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“Accompanying the resumption of human research with the entheogen (psychedelic drug), psilocybin, the range of states of consciousness reported during its action, including both nonmystical and mystical forms of experience, is surveyed and defined. the science and art of facilitating mystical experiences is discussed on the basis of research experience. the potential religious import of these states of consciousness is noted in terms of recognizing the reality of the spiritual, in better understanding the biochemistry of revelation, and in exploring the potentially positive contributions that mystical consciousness may effect in psychological treatment.”
Ruck, C. A. P.. (2014). Entheogens in Ancient Times: Wine and the Rituals of Dionysus. In History of Toxicology and Environmental Health: Toxicology in Antiquity (Vol. 2, pp. 116–125)
Plain numerical DOI: 10.1016/B978-0-12-801506-3.00012-1
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“Entheogen is a neologism used to designate psychoactive substances employed in culturally sanctioned visionary experiences in ritual or religious contexts. the primary divine patron of such experience in classical antiquity was dionysus. his manifestation in the civilized ferment of the grape, which yielded wine, was contrasted with the intoxicants from other sources that preceded viticulture, such as toxic herbs, mushrooms, and animal and insect venoms. emblematic of the contrast was the opposition between the vine and the ivy. the mountain revels of the deity’s female devotees, known as maenads or bacchants, honored the precedents to viticulture in rituals of herb gathering, of which their staff of empowerment, the thyrsus or the narthex, was symbolic. the wine, in contrast, was the drink of the symposium, celebrated by men within the city, with female sexual companions not numbered among the citizenry. the wine itself mediated between the wild and the cultivated in that it was doctored with herbal additives.”
Roberts, T.. (1999). Do entheogen-induced mystical experiences boost the immune system? Psychedelics, peak experiences, and wellness. Advances in Mind-Body Medicine, 9(3), 23–29.
Plain numerical DOI: 10.1054/ambm.1999.0069
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“Daily events that boost the immune system (as indicated by levels of salivary immunoglobulin a), some instances of spontaneous remission, and mystical experiences seem to share a similar cluster of thoughts, feelings, moods, perceptions, and behaviors. entheogens–psychedelic drugs used in a religious context–can also produce mystical experiences (peak experiences, states of unitive consciousness, intense primary religious experiences) with the same cluster of effects. when this happens, is it also possible that such entheogen-induced mystical experiences strengthen the immune system? might spontaneous remissions occur more frequently under such conditions? this article advances the so called ‘emxis hypothesis’–that entheogen-induced mystical experiences influence the immune system.”
Samiy, T.. (
2012). The healing power of dance: A phenomenological study of “being moved” facilitated by the use of entheogens. ProQuest Dissertations and Theses Retrieved from https://tcsedsystem.idm.oclc.org/login?url=https://search.proquest.com/docview/1238204006?accountid=34120%0Ahttp://dg9xu7us4b.search.serialssolutions.com/directLink?&atitle=The+healing+power+of+dance%3A+A+phenomenological+study+of+%22being+moved%22+facili
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“Dance has been an integral aspect of visionary experiences throughout human history. however, little systematic study of descriptions of the phenomenological experience of those participating in entheogen experiences involving movement has been conducted. this study used qualitative methods to explore the lived experience of profound, spontaneous dance/movement, or ‘being moved’, when facilitated by an entheogen. eight participants (3 female and 5 male) were interviewed about their experiences of profound, spontaneous dance/movement. a thematic analysis qualitative research method was used to analyze the transcribed interviews, and revealed eleven higher order themes that describe the experience of profound, spontaneous dance/movement as it arises during an entheogen experience, as follows: (a) encountering and tolerating conflict and overwhelming experience, (b) physical/emotional shifts toward cathartic healing, resolution, and rebirth, (c) emergence of an embodied, creative, ‘true self,’ (d) transcending the ego: spiritual or transpersonal experiences, (e) facilitating (or inhibiting) contextual variables, (f) movements, gestures, and postures, (g) paradox in the experience of being the mover and the moved, (h) entheogens as teachers, (i) entheogens experienced as a sentient life form, (j) entheogens as potentially transformative or traumatic, and (k) phenomenon of dance/movement in context of entheogen use as a developmental process over time. multiple themes were found within each primary category, and primary category 5 had two subcategories. the findings illuminate the qualities of profound, spontaneous dance/movement and how these qualities influence and are influenced by entheogen experiences, as well as the function of ‘being moved’ in the context of entheogen experiences. the researcher proposes that profound, spontaneous dance/movement as it arises during an entheogen experience is represented by diverse components across participants, influenced by the mover’s intention and level of maturity and practice, and that it has multiple possible functions including benefits in healing, creativity, and spiritual or transpersonal development.”
Kovacic, P., & Somanathan, R.. (2009). Novel, unifying mechanism for mescaline in the central nervous system: Electrochemistry, catechol redox metabolite, receptor, cell signaling and structure activity relationships. Oxidative Medicine and Cellular Longevity
Plain numerical DOI: 10.4161/oxim.2.4.9380
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“
A unifying mechanism for abused drugs has been proposed previously from the standpoint of electron transfer. mescaline can be accommodated within the theoretical framework based on redox cycling by the catechol metabolite with its quinone counterpart. electron transfer may play a role in electrical effects involving the nervous system in the brain. this approach is in accord with structure activity relationships involving mescaline, abused drugs, catecholamines and etoposide. inefficient demethylation is in keeping with the various drug properties, such as requirement for high dosage and slow acting.
”
Al-Imam, A.. (2017). The Preferred Terminology Implemented by Psychedelic Users Existing on Online Platforms: A Cross-sectional Analysis. Global Journal of Health Science, 9(11), 140.
Plain numerical DOI: 10.5539/gjhs.v9n11p140
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“
BACKGROUND: the epidemiologic magnitude of the nps (ab)use has been thoroughly explored and geographically mapped in the developed world. however, there are still untapped geographic locations primarily in the developing countries including the middle east. historically, mapping has been done via observational analytics, cross-sectionally and longitudinally, in addition to few experimental studies.materials & methods: the study is cross-sectional; it will implement the internet snapshot technique, in addition to the application of thematic analysis and psychoanalysis of comments of nps (ab)users on the online drug fora and social communication media. the data collected will be analysed for the purpose of concluding a statistical inference in relation to the terms most preferred by substance (ab)users towards hallucinogenic substances.results: the population was dominated by right-handed males; most of which were either heterosexual or bisexual. psychedelics users have a preference for specific terms; psychedelic (73%), entheogen (12%), hallucinogen (11%), spiritual aids (3%), mysticomimetic (1%), psychotomimetic (<1%), medicines (<1%), and trip (<1%). right-handed users who used the term psychedelic were a majority (53%), while right-handed individuals using the terms entheogen and hallucinogen contributed to 8% for each.conclusion: this study is in line with other studies confirming the minute contribution of the middle east to the global nps phenomenon. additional studies are mandatory for different populations including; students, academics and researchers, medical professionals, psychiatric patients, military and para-military organisations, delinquent and prisoners, and even terrorists.
”
MacRae, E.. (1998). Santo Daime and Santa Maria – The licit ritual use of ayabuasca and the illicit use of cannabis in a Brazilian Amazonian religion. International Journal of Drug Policy, 9(5), 325–338.
Plain numerical DOI: 10.1016/S0955-3959(98)00045-0
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“Several brazilian religious groups make controlled ritual use of the indian entheogen ayahuasca, which is legal in the country. but a parallel use of cannabis, by one of these groups faces serious legal obstacles that inhibit the development of ritual controls. the contrast between the licit and ilict use of these substances presents a paradigmatic model of the counterproductive effects of repressive drug leglislation. © 1998 elsevier science b.v. all rights reserved.”
Glockner, J.. (
2012).
Aquí , allá y en todas partes : trascendencia e inmanencia en el uso de enteógenos.
Cuicuilco
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“The discovery of xochipilli’s sculpture in tlalmanalco and the meeting of gordon wasson with maria sabina in huautla de jimenez in the mid-twentieth century reveal us the millenary ritual history of a gender of psychoactive fungi classified as psilocybe by the modern ethnobotany. from the diffusion in the mass media of wasson and his family’s experience, two social phenomena began to develop: on one hand, the massive consumption of this entheogen by young people traveling to the sierra mazateca compelled by simple curiosity or in search of a mystical experience; and by the other hand, the ingestion by some researchers, writers and intellectuals for different purposes, scientific or philosophical, who have communicated this experience trough their work. the article approaches to some of the most relevant aspects of the ritual as an experience of the transcendent and, at the same time, tries to establish some differences and analogies with the experimental practice as an experience of the immanent. (english) [abstract from author]”
Nichols, D. E., Pfister, W. R., Yim, G. K. W., & Cosgrove, R. J.. (1977). A new view of the structural relationship between LSD and mescaline. Brain Research Bulletin
Plain numerical DOI: 10.1016/0361-9230(77)90034-X
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“An examination of the effects of s-(-) and r-(+) 2-amino-1,2,3,4-tetrahydronaphthalene (2-at) on mouse spontaneous activity and rabbit eeg has shown that the s-(-) enantiomer shows selective central effects similar to those of hallucinogens like mescaline. a stereochemical analysis of these results indicates that the structural relationship between mescaline, or other phenethylamine type hallucinogens, may involve correspondence between the aromatic ring of the phenethylamines and the pyrrole portion of the indole nucleus in lsd. © 1977.”
Sewell, R. A.. (
2008).
Unauthorized Research on Cluster Headache.
Entheogen Review,
XVI(4),
117–125.
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“Perhaps the greatest triumph of unauthorized research on visionary plants and drugs to date is the discovery that small doses of lsd, psilocybin, and lsa (lysergic acid amide) are more effective than any conventional medication in treating the dismal disorder, cluster headache. five years ago, no one other than cluster headache patients or neurologists had ever heard of cluster headache.”
Kolp, E., Krupitsky, E., Friedman, H., & Young, M. S.. (
2009).
Entheogen-enhanced transpersonal psychotherapy of addictions: Focus on clinical applications of ketamine for treating alcoholism..
The Praeger International Collection on Addictions, Vol 3: Characteristics and Treatment Perspectives.,
403–417. Retrieved from http://ovidsp.ovid.com/ovidweb.cgi?T=JS&PAGE=reference&D=psyc6&NEWS=N&AN=2009-11518-021
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“Ketamine is an anesthetic that can legally be administered in the united states off-label by a licensed physician for psychiatric treatment as an adjunct to psychotherapy. in this way, it differs from other psychedelics that ate illegal to use in the united states, except in closely controlled research contexts. in subanesthetic doses, ketamine is a psychedelic that reliably induces transpersonal experiences. in addition, ketamine has advantages over other psychedelics due to its rapid onset, safety, and short duration of action. a body of careful scientific research documents that ketamine psychotherapy is effective in the treatment of alcoholism and opioid dependency, as well as to some extent on abused stimulants (e.g., ephedrine). additional data show that ketamine may be successfully used for treating various psychiatric illnesses (e.g., depression, obsessive-compulsive disorder, posttraumatic stress disorder, and phobias), some personality disorders (e.g., avoidant and histrionic personality disorder), and also some psychosomatic illnesses (e.g., tension headaches and ulcerative colitis). these studies demonstrate impressive benefits for many clients who showed improvements after receiving ketamine, including becoming more responsible, emotionally mature and open, self-confident and self-sufficient, and having increased ego strength and less anxiety and depression. in addition to these many benefits, clients often experienced both existential and spiritual growth. these transformations may reinforce positive attitudes toward sobriety and healthy lifestyles that supported stable recovery from alcohol and substance use disorders. continued scientific research on ketamine in well-controlled studies is indicated now because of its demonstrated therapeutic effectiveness, biological safety, and pragmatic availability as one of the few legally available psychedelics and the only one that has shown clinical value. (psycinfo database record (c) 2009 apa, all rights reserved)”
Carstairs, S. D., & Cantrell, F. L.. (2010). Peyote and mescaline exposures: A 12-year review of a statewide poison center database. Clinical Toxicology
Plain numerical DOI: 10.3109/15563650903586745
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“Medical usage is briefly discussed, case studies of use and potential negative effects are discussed background: peyote, a cactus containing the hallucinogen mescaline, has been used by native americans for thousands of years. illicit use is also known to occur, but reports in the medical literature consist only of isolated case reports. objectives . we sought to identify characteristics of patients with reported exposure to peyote or mescaline. methods . we performed a retrospective review of the california poison control system database for the years 1997–2008 for all cases of single-substance human exposure using the search terms ‘peyote’ and ‘mescaline.’ results: there were a total of 31 single-substance exposures to peyote or mescaline. thirty (97%) exposures were intentional; 30 (97%) exposures were through the oral route, whereas one patient (3%) insufflated mescaline powder. five patients (16%) were managed at home, whereas the remainder patients were managed in a healthcare facility. commonly reported effects included hallucinations, tachycardia, agitation, and mydriasis. vomiting was reported in only one case. conclusions: although uncommonly encountered, use of peyote and mescaline was associated with clinically significant effects requiring treatment in a substantial number of patients. clinical effects were usually mild or moderate, and life-threatening toxicity was not reported in this case series.”
Helminiak, D. A.. (2010). “Theistic psychology and psychotherapy”: A theological and scientific critique. Zygon, 45(1), 47–74.
Plain numerical DOI: 10.1111/j.1467-9744.2010.01058.x
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“I take the apa publication a spiritual strategy for counseling and psychotherapy (richards and bergin 2005), along with a devoted issue of journal of psychology and theology (nelson and slife 2006), as a paradigmatic example of a trend. other instances include the uncritical use of ‘eastern’ philosophy in humanistic and trans- personal psychology, almost normative appeal to the ‘sacred’ within the psychology of spirituality, talk of ‘god in the brain’ within neuro- logical research, the neologism entheogen referring to psychedelic drugs, and calls for new specializations such as neurotheology and theobiology. in response to the legitimate ethical requirements of respect and open- ness regarding clients’ religious worldviews, the trend is to make god an essential component in psychological theory. the argument is that god is active in the universe and especially in human affairs to such an extent that any accurate account of strictly psychological matters, not just a comprehensive, interdisciplinary purview that could in- clude a distinct theological dimension, must include god as an ex- planatory factor. less nuanced than standard theological thought about divine intervention—including a range of opinions from su- pernaturalism, to occasionalism, to providential and deistic natural- ism—this trend would blur the epistemological differences between religion and science by appeal to claimed knowledge sources such as inspiration and revelation and thus undermine the achievements of evidence-based science and establish particularistic religious beliefs as standard explanatory accounts. the concern to include a spiritual, in contrast to a religious or theist, dimension in psychological theory is welcome; but elaborated approaches, such as my own and those of roberto assagioli, viktor frankl, and ken wilber, open to varied theological applications, already exist.”
R.K., O.. (
1972).
Mescaline.
Texas Medicine
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“Mescaline, or 3,4,5 trimethoxyphenylethylamine, is one of the eight alkaloids present in peyote. mescaline is a psychedelic, or a hallucinogen; as such, it has effects similar to those of other hallucinogens, with dosage and duration of action being the primary variables among the different compounds. mescaline is the least potent of the commonly used hallucinogens in that it requires the largest dose to be effective, but it is slightly longer acting than even lsd. although pure mescaline is not likely to be purchased off the street, it has not yet been indicted for having adverse effects in nonpregnant animals other than the possibility of producing effects of nonspecific stress; during pregnancy the probability exists that a single normal dose of mescaline might contribute to congenital malformations, miscarriages, or stillbirths.”
Ott, J.. (
1995). Ethnopharmacognosy and human pharmacology of Salvia divinorum and salvinorin A. Curare (Vol. 18) Retrieved from http://cat.inist.fr/?aModele=afficheN&cpsidt=3293920
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“After a thorough review of the limited ethnographic data on shamanic use of the entheogenic mint « salvia divinorum » by the mazatec indians of the sierra madre oriental of the mexican state of oaxaca, with special emphasis on pharmacognostical aspects, the a. details the phytochemical studies which led to the isolation of the novel diterpene salvinorin a in 1982-1984. « lingering » doubts as to the visionary properties of this compound were laid to rest a decade later, when « basement shamans » in the usa isolated and tested the compound in psychonautic bioassays. a tabular summary of 60 trials is presented ; documenting activity of infusions of « salvia divinorum » leaves in water, of the fresh leaves chewed, whether swallowed or retained in the mouth, and of the dried leaves smoked. pharmacological activity of salvinorin a in human volunteers is likewise discussed, both for inhalation of the vaporized compound and sublingual application of 1% solutions in acetone or dmso ; including original research here reported. extremely low thresholds for psychoactivity of salvinorin a show this compound to be the most potent natural product entheogen known ; some 10 times the potency of psilocybine from mushrooms likewise used as shamanic inebriants by the huichol, tarahumara and other indigenous peoples of northern mexico. speculations regarding the status of « salvia divinorum » as a cultigen are discussed. an exhaustive bibliography reviews the literature on this inebriant”
Shulgin, A. T., & Carter, M. F.. (
1975).
Centrally Active Phenethylamines.
Psychopharmacology Communications
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“The two-carbon homologs of two potent psychotomimetic agents are described. unlike the parent isopropylamine compounds (4-methyl-2,5-dimethoxyamphetamine, dom, stp; and 4-bromo-2,5-dimethoxyamphetamine, pbr, 4-br) these phenethylamines lead to an intoxication state which is, in normal subjects, of short duration and of greatly increased sensory enhancement, but which does not superimpose hallucinogenesis. these two phenethylamines, 4-methyl-2,5-dimethoxyphenethylamine (ii) and 4-bromo-2,5-dimethoxyphenethylamine (iii), are active in man at oral levels of 0.1 to 0.2 mg/kg, approximately one tenth the potency of their three-carbon counterparts.”
El-Seedi, H. R., De Smet, P. A. G. M., Beck, O., Possnert, G., & Bruhn, J. G.. (2005). Prehistoric peyote use: Alkaloid analysis and radiocarbon dating of archaeological specimens of Lophophora from Texas. Journal of Ethnopharmacology
Plain numerical DOI: 10.1016/j.jep.2005.04.022
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“Two archaeological specimens of peyote buttons, i.e. dried tops of the cactus lophophora williamsii (lem.) coulter, from the collection of the witte museum in san antonio, was subjected to radiocarbon dating and alkaloid analysis. the samples were presumably found in shumla cave no. 5 on the rio grande, texas. radiocarbon dating shows that the calibrated 14c age of the weighted mean of the two individual dated samples corresponds to the calendric time interval 3780-3660 bc (one sigma significance). alkaloid extraction yielded approximately 2% of alkaloids. analysis with thin-layer chromatography (tlc) and gas chromatography-mass spectrometry (gc-ms) led to the identification of mescaline in both samples. no other peyote alkaloids could be identified. the two peyote samples appear to be the oldest plant drug ever to yield a major bioactive compound upon chemical analysis. the identification of mescaline strengthens the evidence that native north americans recognized the psychotropic properties of peyote as long as 5700 years ago. © 2005 elsevier ireland ltd. all rights reserved.”
Rickli, A., Moning, O. D., Hoener, M. C., & Liechti, M. E.. (2016). Receptor interaction profiles of novel psychoactive tryptamines compared with classic hallucinogens. European Neuropsychopharmacology
Plain numerical DOI: 10.1016/j.euroneuro.2016.05.001
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“The present study investigated interactions between the novel psychoactive tryptamines dipt, 4-oh-dipt, 4-oh-met, 5-meo-amt, and 5-meo-mipt at monoamine receptors and transporters compared with the classic hallucinogens lysergic acid diethylamide (lsd), psilocin, n,n-dimethyltryptamine (dmt), and mescaline. we investigated binding affinities at human monoamine receptors and determined functional serotonin (5-hydroxytryptamine [5-ht]) 5-ht2aand 5-ht2breceptor activation. binding at and the inhibition of human monoamine uptake transporters and transporter-mediated monoamine release were also determined. all of the novel tryptamines interacted with 5-ht2areceptors and were partial or full 5-ht2aagonists. binding affinity to the 5-ht2areceptor was lower for all of the tryptamines, including psilocin and dmt, compared with lsd and correlated with the reported psychoactive doses in humans. several tryptamines, including psilocin, dmt, dipt, 4-oh-dipt, and 4-oh-met, interacted with the serotonin transporter and partially the norepinephrine transporter, similar to 3,4-methylenedioxymethamphetamine but in contrast to lsd and mescaline. lsd but not the tryptamines interacted with adrenergic and dopaminergic receptors. in conclusion, the receptor interaction profiles of the tryptamines predict hallucinogenic effects that are similar to classic serotonergic hallucinogens but also mdma-like psychoactive properties.”
Nichols, D. E., Jadhav, K. P., Oberlender, R. A., Zabik, J. E., Bossart, J. F., Hamada, A., & Miller, D. D.. (1984). Synthesis and Evaluation of Substituted 2-Phenylcyclobutylamines as Analogues of Hallucinogenic Phenethylamines: Lack of LSD-like Biological Activity. Journal of Medicinal Chemistry
Plain numerical DOI: 10.1021/jm00375a004
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“Cis- and trans-2-(2,4,5-trimethoxyphenyl)cyclobutylamine and trans-2-(2,5-dimethoxy-4-methylphenyl)cyclobutylamine were synthesized as conformationally restricted analogues of hallucinogenic phenylisopropylamines. in rats trained to discriminate saline from lsd (0.08 mg/kg, ip) in a two-lever drug discrimination paradigm, no generalization of the lsd stimulus to the cis trimethoxy compound occurred at doses up to 20 mg/kg. for both of the trans compounds, partial generalization of the lsd cue occurred at doses of 5 mg/kg or greater. in contrast, complete generalization occurred with trans-2-(2,5-dimethoxy-4-methylphenyl)cyclopropylamine. the ed50 for this compound and the doses of the trans cyclobutyl homologues at which significant drug-appropriate responding occurred indicate that the latter are on the order of 50-75 times less potent than the cyclopropylamine analogue. the lack of generalization to the cyclobutylamines indicates either that their discriminative stimulus properties differ from lsd or that they lack discriminative effects.”
Deneau, G., Yanagita, T., & Seevers, M. H.. (1969). Self-administration of psychoactive substances by the monkey. Psychopharmacologia
Plain numerical DOI: 10.1007/BF00405254
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“A method has been developed which permits monkeys to self-ad-minister drug solutions, at will, through indwelling intravenous catheters. psycho-logical dependence on the effects of a drug occurs when a naive monkey voluntarily initiates and maintains self-administration of the drug. if, in addition to psycho-logical dependence, the drug also produces psychotoxieity, either directly or upon abrupt withdrawal, it has a potential abuse liability. in the present study monkeys developedpsychological dependence on morphine, codeine, cocaine, d-amphetamine, pentobarbital, ethanol, and caffeine. all of these drugs except caffeine produced psychotoxicity. monkeys did not develop psycho-logical dependence on nalorphine, morphinc-nalorphine mixtures, chlorpromazine, mescaline or physiological saline.”
Schoenfeld, R. I.. (1976). Lysergic acid diethylamide- and mescaline-induced attenuation of the effect of punishment in the rat. Science
Plain numerical DOI: 10.1126/science.1063447
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“At a dose as low as 1 microgram per kilogram of body weight, lysergic acid diethylamide (lsd) significantly decreased the suppressive effect of electric shock on licking behavior of the rat. attenuation of punishment was also obtained with mescaline, but neither dimethyltryptamine nor delta9-tetrahydrocannabinol was active in this test. cyproheptadine and alpha-propyldopacetamide, drugs that interfere with the function of neurons that contain serotonin, have a behavioral effect similar to that of lsd and mescaline, which suggests that the attenuation of punishment produced by these hallucinogens may result from decreased activity of such neurons.”
Tupper, K. W.. (
2009).
Entheogenic Healing: The Spiritual Effects And Therapeutic Potential Of Ceremonial Ayahuasca Use Retrieved from http://kentupper.com/resources/HPoS+Entheogenic+Healing+Chapter+-+December+2009.pdf
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“The overlap between the fields of health and spirituality is well illustrated by traditions of entheogenic healing, and in particular the transnational sociological trend of ceremonial ayahuasca drinking. entheogenic healing is a concept that derives from the term ‘entheogen,’ coined by scholars to convey the sacramental nature of traditional shamanic practices using psychoactive plants (ruck, bigwood, staples, ott, & wasson, 1979). ayahuasca is a decoction characteristically prepared from a boiled mash of a jungle liana (banisteriopsis caapi) and a common admixture leaf (psychotria viridis). the unique pharmacological synergy between particular chemicals in these plants produces a profound altered state of consciousness in humans. ayahuasca is most commonly consumed in ritual contexts, both in traditional amazonian indigenous practices and, of late, in various (post)modern syncretistic spiritual or hybrid healing practices. this chapter briefly reviews the renaissance of interest in the potential therapeutic value of substances known as psychedelics or entheogens1 , and explores the concept of entheogenic healing with examples from various forms of ayahuasca drinking. it covers traditional and modern practices of using ayahuasca in ritual contexts—including indigenous amazonian traditions and more modern hybrid forms, such as syncretistic brazilian ayahuasca churches—to diagnose and treat illnesses. it considers the importance of ritual, especially the element of music, for ayahuasca healing. finally, it looks at addiction as a type of psychospiritual illness for which entheogenic healing with ayahuasca may be particularly well suited.”
Tupper, K. W.. (2009). Ayahuasca healing beyond the Amazon: The globalization of a traditional indigenous entheogenic practice. Global Networks, 9(1), 117–136.
Plain numerical DOI: 10.1111/j.1471-0374.2009.00245.x
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“Ayahuasca commonly refers to a psychoactive amazonian indigenous brew traditionally used for spiritual and healing purposes (that is as an entheogen). since the late twentieth century, ayahuasca has undergone a process of globalization through the uptake of different kinds of socio-cultural practices, including its sacramental use in some new brazilian religious movements and its commodified use in cross-cultural vegetalismo practices, or indigenous-style rituals conducted primarily for non-indigenous participants. in this article, i explore the rise of such rituals beyond the amazon region, and consider some philosophical and political concerns arising from this novel trend in ayahuasca use, including the status of traditional indigenous knowledge, cultural appropriation, and intellectual property. i discuss a patent dispute in the united states and allegations of biopiracy related to ayahuasca. i conclude the article with some reflections on the future of ayahuasca drinking as a transnational sociological phenomenon.”
Aragane, M., Sasaki, Y., Nakajima, J., Fukumori, N., Yoshizawa, M., Suzuki, Y., … Nagumo, S.. (2011). Peyote identification on the basis of differences in morphology, mescaline content, and trnL/trnF sequence between Lophophora williamsii and L. diffusa. Journal of Natural Medicines
Plain numerical DOI: 10.1007/s11418-010-0469-7
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“Genus lophophora (cactaceae) has two species: lophophora williamsii coulter, which is called peyote, and l. diffusa bravo. although it was reported that l. williamsii contained mescaline and l. diffusa did not, we found l. williamsii specimens that did not contain mescaline. this finding indicated that the two species could not be differentiated in terms of mescaline content. moreover, the relationship between mescaline content and morphology of the two species is also unknown. in this study, we attempted to clarify the difference in morphology, mescaline content, and dna alignment of the chloroplast trnl/trnf region between l. williamsii and l. diffusa. as a result, l. williamsii specimens were classified into two groups. group 1 had small protuberances on the epidermis, contained mescaline, and the analyzed region on the trnl/trnf sequence was 881 base pairs (bp) long in all except one (877 bp). group 2 had large protuberances on the epidermis, did not contain mescaline, and the analyzed region was 893 bp long. on the other hand, l. diffusa had medium-sized protuberances on the epidermis, did not contain mescaline, and the analyzed region was 903 bp long. also investigated was the potential application of the pcr-restriction fragment length polymorphism (rflp) method as a means of identification based on the trnl/trnf sequence. by applying the pcr-rflp method, the two species could be distinguished and l. williamsii specimens could be differentiated into group 1 and group 2.”
Johnstad, P. G.. (2018). Powerful substances in tiny amounts: An interview study of psychedelic microdosing. NAD Nordic Studies on Alcohol and Drugs, 35(1), 39–51.
Plain numerical DOI: 10.1177/1455072517753339
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“Aims:this article presents a qualitative interview study of people who microdose with psychedelic drugs, which means that the user takes about one tenth of an ordinary recreational dose.design:respondents (n = 21) were recruited at several internet fora for individual interviews via private messaging. every participant was male, and the median respondent was in his 30s with a stable job and relationship and extensive entheogen experience.results:respondents tended to experiment with microdosing in phases, reporting mostly positive consequences from this form of drug use. reported effects included improved mood, cognition, and creativity, which often served to counteract symptoms especially from conditions of anxiety and depression. there were also reports of various challenges with psychedelic microdosing, and some did not find the practice worth continuing.conclusion:the study obtained evidence of a group of users taking small doses of psychedelics not for the purpose of intoxication but to enhance every…”
Krebs, T. S., & Johansen, P.-Ø.. (2013). Psychedelics and Mental Health: A Population Study. PLoS ONE, 8(8), e63972.
Plain numerical DOI: 10.1371/journal.pone.0063972
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“BACKGROUND: the classical serotonergic psychedelics lsd, psilocybin, mescaline are not known to cause brain damage and are regarded as non-addictive. clinical studies do not suggest that psychedelics cause long-term mental health problems. psychedelics have been used in the americas for thousands of years. over 30 million people currently living in the us have used lsd, psilocybin, or mescaline. objective: to evaluate the association between the lifetime use of psychedelics and current mental health in the adult population. method: data drawn from years 2001 to 2004 of the national survey on drug use and health consisted of 130,152 respondents, randomly selected to be representative of the adult population in the united states. standardized screening measures for past year mental health included serious psychological distress (k6 scale), mental health treatment (inpatient, outpatient, medication, needed but did not receive), symptoms of eight psychiatric disorders (panic disorder, major depressive episode, mania, social phobia, general anxiety disorder, agoraphobia, posttraumatic stress disorder, and non-affective psychosis), and seven specific symptoms of non-affective psychosis. we calculated weighted odds ratios by multivariate logistic regression controlling for a range of sociodemographic variables, use of illicit drugs, risk taking behavior, and exposure to traumatic events. results: 21,967 respondents (13.4% weighted) reported lifetime psychedelic use. there were no significant associations between lifetime use of any psychedelics, lifetime use of specific psychedelics (lsd, psilocybin, mescaline, peyote), or past year use of lsd and increased rate of any of the mental health outcomes. rather, in several cases psychedelic use was associated with lower rate of mental health problems. conclusion: we did not find use of psychedelics to be an independent risk factor for mental health problems.”
Hermle, L., Fünfgeld, M., Oepen, G., Botsch, H., Borchardt, D., Gouzoulis, E., … Spitzer, M.. (1992). Mescaline-induced psychopathological, neuropsychological, and neurometabolic effects in normal subjects: Experimental psychosis as a tool for psychiatric research. Biological Psychiatry
Plain numerical DOI: 10.1016/0006-3223(92)90059-9
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“The psychological, neuropsychological, and neurometabolic effects of the hallucinogenic agent mescaline were investigated in 12 normal men who were volunteers. mescaline produced an acute psychotic state 3 1 2-4 hr after drug intake, as measured by the brief psychiatric rating scale (bprs) and paranoid depression scale (pds). the assessment of altered states of consciousness (apz) questionnaire revealed specific effects of mescaline in the visual system. neuropsychological effects were studied with a face/nonface decision task with known right-hemisphere advantage, in which mescaline induced a decrease of functioning of the right hemisphere. in functional brain imaging using single photon emission computed tomography (spect), mescaline produced a ‘hyperfrontal’ pattern with an emphasis on the right hemisphere, which was correlated with mescaline-induced psychotic psychopathology. our findings question the validity of the concept of hypofrontality as an explanation for schizophrenic symptomatology. the study of psychoactive substances under controlled laboratory conditions has the methodological advantage of intraindividual control, and hence, minimal variability of data. © 1992.”
Barnard, W. W.. (2014). Entheogens in a religious context: The case of the santo daime religious tradition. Zygon, 49(3), 666–684.
Plain numerical DOI: 10.1111/zygo.12109
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“This essay first draws upon the work of william james and others to propose a nonphysicalistic understanding of the relationship between the brain and consciousness in order to articulate a philosophical perspective that can understand entheogenic visionary/ mystical experiences as something other than hallucinations. it then focuses on the santo daime tradition, a religious movement that began in brazil in the early part of the twentieth century, to provide an example of the personal and social ramifications of taking an entheogen (ayahuasca) within a disciplined religious context. the essay claims that the santo daime is one example of a contemporary mystery school; gives a brief history of the development of this religion; discusses the key theological assumptions of this movement; investigates the important role played by visionary/mystical experiences within this religion; underscores the centrality of healing and spiritual transformation for members of this tradition; and ends with an examination of the crucial significance of spiritual discipline within this entheogenically based religion. [abstract from author] copyright of zygon: journal of religion & science is the property of wiley-blackwell and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder’s express written permission. however, users may print, download, or email articles for individual use. this abstract may be abridged. no warranty is given about the accuracy of the copy. users should refer to the original published version of the material for the full abstract. (copyright applies to all abstracts.)”
Braden, M. R., Parrish, J. C., Naylor, J. C., & Nichols, D. E.. (2006). Molecular Interaction of Serotonin 5-HT2A Receptor Residues Phe339(6.51) and Phe340(6.52) with Superpotent N-Benzyl Phenethylamine Agonists. Molecular Pharmacology
Plain numerical DOI: 10.1124/mol.106.028720
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“Experiments were conducted to examine the molecular basis for the high affinity and potency of a new class of 5-ht2a receptor agonists, n-benzyl phenethylamines. competition binding assays at several serotonin receptors confirmed that an n-arylmethyl substitution was necessary for affinity increases up to 300-fold over simple n-alkyl homologs, as well as enhanced selectivity for 5-ht2a versus 5-ht2c and 5-ht1a receptors. pi hydrolysis functional assays confirmed that these n-benzyl phenethylamines are potent and highly efficacious agonists at the rat 5-ht2a receptor. virtual docking of these compounds into a human 5-ht2a receptor homology model indicated that the n-benzyl moiety might be interacting with phe339(6.51), whereas the phenethylamine portion was likely to be interacting with phe340(6.52). experiments in h5-ht2a receptors with phe339(6.51)l and phe340(6.52)l mutations seem to support this hypothesis. dramatic detrimental effects on affinity, potency, and intrinsic activity were observed with the phe339(6.51)l mutation for all n-benzyl analogs, whereas most n-unsubstituted phenethylamines and traditional agonists were only weakly affected, if at all. consistent with other published studies, the phe340(6.52)l mutation detrimentally affected affinity, potency, and intrinsic activity of nearly all compounds tested, although a strong change in intrinsic activity was not seen with most n-aryl analogs. these data further validate the topology of our h5-ht2a receptor homology model. it is noteworthy that this study is the first to identify a hitherto unrecognized role for residue 6.51 in agonist activation of a serotonin g protein-coupled receptor (gpcr), whereas most previous reports have suggested a varied and sometimes contradictory role in homologous gpcrs. the american society for pharmacology and experimental therapeutics”
Johnstad, P. G.. (2018). Powerful substances in tiny amounts: An interview study of psychedelic microdosing. NAD Nordic Studies on Alcohol and Drugs, 35(1), 39–51.
Plain numerical DOI: 10.1177/1455072517753339
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“Aims:this article presents a qualitative interview study of people who microdose with psychedelic drugs, which means that the user takes about one tenth of an ordinary recreational dose.design:respondents (n = 21) were recruited at several internet fora for individual interviews via private messaging. every participant was male, and the median respondent was in his 30s with a stable job and relationship and extensive entheogen experience.results:respondents tended to experiment with microdosing in phases, reporting mostly positive consequences from this form of drug use. reported effects included improved mood, cognition, and creativity, which often served to counteract symptoms especially from conditions of anxiety and depression. there were also reports of various challenges with psychedelic microdosing, and some did not find the practice worth continuing.conclusion:the study obtained evidence of a group of users taking small doses of psychedelics not for the purpose of intoxication but to enhance every…”
Kyzar, E. J., Collins, C., Gaikwad, S., Green, J., Roth, A., Monnig, L., … Kalueff, A. V.. (2012). Effects of hallucinogenic agents mescaline and phencyclidine on zebrafish behavior and physiology. Progress in Neuro-Psychopharmacology and Biological Psychiatry
Plain numerical DOI: 10.1016/j.pnpbp.2012.01.003
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“Mescaline and phencyclidine (pcp) are potent hallucinogenic agents affecting human and animal behavior. as their psychotropic effects remain poorly understood, further research is necessary to characterize phenotypes they evoke in various animal models. zebrafish (danio rerio) are rapidly emerging as a new model organism for neuroscience research. here, we examine the effects of mescaline (5-20. mg/l) and pcp (0.5-3. mg/l) in several zebrafish paradigms, including the novel tank, open field and shoaling tests. mescaline and pcp dose-dependently increased top activity in the novel tank test, also reducing immobility and disrupting the patterning of zebrafish swimming, as assessed by ethograms. pcp, but not mescaline, evoked circling behavior in the open field test. at the highest doses tested, mescaline markedly increased, while pcp did not affect, zebrafish shoaling behavior. finally, 20. mg/l mescaline did not alter, and 3. mg/l pcp elevated, whole-body cortisol levels. overall, our studies indicate high sensitivity of zebrafish models to hallucinogenic compounds with complex behavioral and physiological effects. © 2012 elsevier inc.”
Roberts, T. B. [Ed]. (
2001).
Psychoactive sacramentals: Essays on entheogens and religion..
Psychoactive Sacramentals: Essays on Entheogens and Religion.
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“(From the cover) this book examines the place that psychoactive sacramentals–entheogens–have in contemporary religions and religions of the future. the contributing authors discuss entheogens as powerful tools for opening minds and contend that they are spiritual tools among many. topics discussed include: (1) how the use of entheogens can aid in spiritual development, (2) how entheogens can enhance spiritual practices, and (3) cautions that ought to be considered regarding entheogen use. (psycinfo database record (c) 2012 apa, all rights reserved)”
De Silva, R., Nikitin, N. P., Bhandari, S., Nicholson, A., Clark, A. L., & Cleland, J. G. F.. (2005). Atherosclerotic renovascular disease in chronic heart failure: Should we intervene?. European Heart Journal, 26(16), 1596–1605.
Plain numerical DOI: 10.1093/eurheartj/ehi304
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“Renal artery stenosis (ras) is most commonly caused by atherosclerosis, which is also the most common cause of chronic heart failure (chf). one-third of patients with chf are reported to have significant renovascular disease. the presence of ras confers a worse outcome in studies of hypertension and coronary disease, though data are lacking for patients with chf. as the kidney is intricately involved in the fluid retention that occurs in chf, an adverse effect of ras on outcome would be expected. presentations of ras in chf include flash pulmonary oedema, hypertension, worsening of chf, and worsening renal function. ras commonly progresses and may cause worsening of renal function in patients with chf and previously stable renal function. a variety of investigations that can safely and accurately identify ras in chf are available, although none is recommended in current guidelines for the management of chf. treatment for ras, whether for hypertension, for renal dysfunction, or for pulmonary oedema, is at the discretion of the physician due to the lack of adequate randomized controlled trials demonstrating the efficacy and safety of intervention. as it is not clear how ras should be managed in chf, screening cannot be advocated. currently, a multicentre randomized outcome trial, which includes a cohort of patients with ras and chf, is in progress to provide answers in this area of uncertainty.”
Doyle, R.. (2012). Healing with Plant Intelligence: A Report from Ayahuasca. Anthropology of Consciousness, 23(1), 28–43.
Plain numerical DOI: 10.1111/j.1556-3537.2012.01055.x
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“Numerous and diverse reports indicate the efficacy of shamanic plant adjuncts (e.g., iboga, ayahuasca, psilocybin) for the care and treatment of addiction, post-traumatic stress disorder, cancer, cluster headaches, and depression. this article reports on a first-person healing of lifelong asthma and atopic dermatitis in the shamanic context of the contemporary peruvian amazon and the sometimes digital ontology of online communities. the article suggests that emerging language, concepts, and data drawn from the sciences of plant signaling and behavior regarding ‘plant intelligence’ provide a useful heuristic framework for comprehending and actualizing the healing potentials of visionary plant ‘entheogens’ (wasson 1971) as represented both through firstperson experience and online reports. together with the paradigms and practices of plant signaling, biosemiotics provides a robust and coherent map for contextualizing the often reported experience of plant communication with ayahuasca and other entheogenic plants. the archetype of the ‘plant teachers’ (called doctores in the upper amazon) is explored as a means for organizing and interacting with this data within an epistemology of the “hallucination/ perception continuum (fischer 1975). ‘ecodelic’ is offered as a new linguistic interface alongside ‘entheogen’ (wasson 1971).”
Saldaña Ramírez, A.. (
2013).
En busca de la cura: Prácticas adivinatorias y terapéuticas entre los nahuas del Alto Balsas (Guerrero) presentes en Morelos.
Cuicuilco,
20(56),
203–222.
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“This article analyzes a divination process known as ‘the raffle’ (‘la rifa’) and some therapeutic, ritual practices among the people from two nahua communities in alto balsas, guerrero, many of whom now live in the state of morelos. the objective is to show the different ways in which the residents of tula del río and san agustín oapan deal with their health problems, while immersed in a complex of practices pertaining to the logics of different cultures. the ailments emphasized are basically those related to fright (espanto), which involves the ‘raising of the soul/shades;’ witchcraft that calls for a treatment based on drinking the ‘cure’ prepared on the basis of an entheogen. other sicknesses, which are considered to be those that should be ‘treated by a doctor,’ are also viewed.”
Gewirtz, J. C., & Marek, G. J.. (2000). Behavioral evidence for interactions between a hallucinogenic drug and group II metabotropic glutamate receptors. Neuropsychopharmacology
Plain numerical DOI: 10.1016/S0893-133X(00)00136-6
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“Recent electrophysiological studies in our laboratory have demonstrated a physiological interaction between 5-ht(2a) and metabotropic glutamate 2/3 (mglu2/3) receptors in the medial prefrontal cortex. several behavioral studies have found that phenethylamine hallucinogens with partial agonist activity at 5-ht(2a) receptors induce head shakes when directly administered into the medial prefrontal cortex. the purpose of the present experiments was to examine whether an interaction occurs between mglu2/3 and 5-ht(2a) receptors on a behavioral level using head shakes induced by phenethylamine hallucinogens as a model of 5-ht(2a) receptor activation. administration of the mglu2/3 agonist ly354740 (0.3-10 mg/kg, ip) suppressed head shakes induced by the phenethylamine hallucinogen 1-(2,5-dimethoxy-4-iodophenyl)-2- aminopropane (doi). conversely, administration of the mglu2/3 antagonist ly341495 (1 mg/kg, ip) enhanced the frequency of doi-induced head shakes. taken together, these results raise the possibility that the psychomimetic properties of hallucinogenic drugs may be mediated in part, via increased glutamate release following activation of 5-ht(2a) receptors. (c) 2000 american college of neuropsychopharmacology.”
Glass-Coffin, B.. (2010). Shamanism and San Pedro through Time: Some notes on the archaeology, history, and continued use of an entheogen in northern Peru. Anthropology of Consciousness, 21(1), 58–82.
Plain numerical DOI: 10.1111/j.1556-3537.2010.01021.x
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“This paper discusses archaeological, historical, and contemporary ethnographic evidence for the use of the san pedro cactus in northern peru as a vehicle for traveling between worlds and for imparting the vista (magical sight) necessary for shamanic healers to divine the cause of their patients ailments. using iconographic, ethnohistorical, and ethnographic evidence for the uninterrupted use of this sacred plant as a means of access to the divine and as a tool for healing, it describes the relationship between san pedro, ancestor worship, water/ fertility cults and also the common symbolic associations between san pedro and wind-spirits. it closes by suggesting that the more than 2000 year time-depth of using this plant as a means for accessing the realms of spirit and as a tool for healing should serve to challenge the unfortunate tendency in the contemporary united states to consider this plant as a recreational drug.”
García Quintanilla, A., & Eastmond Spencer, A.. (
2012).
Rituales de la x-táabentun (Turbina corymbosa) y de los mayas yucatecos. (Spanish).
Revista Cuicuilco,
19(53),
257–281. Retrieved from http://www.scielo.org.mx/pdf/cuicui/v19n53/v19n53a12.pdf%0Ahttp://search.ebscohost.com/login.aspx?direct=true&db=a9h&AN=89173406&lang=es&site=ehost-live
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“Turbina corymbosa grows throughout mesoamerica, it is widely known in yucatan and has no spanish name. it’s known by its maya name as xtabentun or, correctly spelt, x-táabentun. many hypotheses have been put forward regarding its ritual use but the yucatecan mayas have been especially reserved about this. based on contemporary oral tradition, we can now distinguish two types of ritual management of the plant: the first has to do with rituals performed by the x-táabentun itself, together with other plants from the convolvulaceae family. the second type is carried out by humans. according to testimonials collected in pixoy, yucatan, it is clear that the villagers are aware of the hallucinogenic properties of the x-táabentun seeds (when the plant is colonized by a fungus from the clavicipitaceae family); and that the midwives also know of the therapeutic value of the alkaloids produced by these (colonized) plants. following on from this knowledge, we analyze accounts that have been kept in the collective memory about plants, drinks and seeds, as well as colonial sources that refer to substances used by shamans. finally we present our identification of a x-táabentun flowering plant on a maya vase from the classical period, and we revisit thompson’s [1998] and de la garza’s [1990] hypotheses about the existence amongst the ancient maya elite of a profound knowledge of this native plant and its use as a entheogen in ancient times (english) [abstract from author]”
Dunne, P.. (
1989).
San Pedro morning.
American Birds,
43,
1251-1253 ST-San Pedro morning.
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“The plant san pedro, botanically known as trichocereus pachanoi, or as echinopsis pachanoi, originally comes from the slopes of the andean mountains. it is a cactus that does not grow well in the rainforest, other than in cultivated gardens, and is therefore not traditionally used by the uwishin. but many of them know and use this entheogen in their practice as a side-aid to natem, obtaining it as a powder or as a liquid from their andean peers and revering it as much as any other sacred plant medicine. because you will one day probably encounter it on your plant medicine adorned path, and because on my path i had some of my most profound experiences journeying with the san pedro, i felt it deserved a chapter on its own. san pedro is a columnar cactus with little to no spines. it can grow up to six metres tall, but most mature specimens that i have seen in the wild were no higher than four metres. it usually has six or seven ribs, but it can be as many as thirteen. at home i have a rare san pedro which has four ribs, a number that, according to many indigenous shamans, gives the plant special powers, as the number of ribs correlates with the four directions. sometimes it has white flowers that only appear at night, and on sporadic occasions it grows tasteful red fruit. the cactus can be found everywhere in the andean region, with a specific abundance in the highlands of ecuador and peru. it is an incredibly fast growing cactus. if cultivated in a sunny and dry climate, and regularly watered, it can grow up to half a metre per year. the san pedro cactus contains many different alkaloids but the most interesting component is mescaline. mescaline is a psycho-active substance that can also be found in various other members of the echinopsis genus, including san pedro’s tinier bigger brother, the peyote. however, the varying alkaloid combinations in these different species all give a different experience on top of that basic energy that the mescaline gives. as such, the specific mix of alkaloids follows the energy, or spirit, of the specific plant at a non-physical level. the reason for these cacti to develop biosynthesis of mescaline within their evolutionary path is because it functions as a stress response agent, pretty similar to how stress response mechanisms function in the animal kingdom. but besides internal signalling, mescaline also protects the cells of the plant against degradation from invading organisms. as such i am not surprised that most of …”
Zhang, C., & Marek, G. J.. (2008). AMPA receptor involvement in 5-hydroxytryptamine2Areceptor-mediated pre-frontal cortical excitatory synaptic currents and DOI-induced head shakes. Progress in Neuro-Psychopharmacology and Biological Psychiatry
Plain numerical DOI: 10.1016/j.pnpbp.2007.07.009
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“Glutamate plays an important role in the psychotomimetic effects of both channel blocking n-methyl d-aspartate (nmda) receptor antagonists and hallucinogenic drugs which activate 5-hydroxytryptamine2a(5-ht2a) receptors. previous work suggested that activation of non-nmda ionotropic glutamate receptors mediates the effects of 5-ht-induced excitatory post-synaptic potentials/currents (epsps/epscs) when recording from layer v pyramidal cells in the rat medial pre-frontal cortex (mpfc). however, those effects are mediated by either α-amino-3-hydroxy-5-methylisoxazole-4-propionate (ampa) or kainate receptors of the igluk5 subtype. to test whether activation of ampa receptors is sufficient to mediate 5-ht-induced epscs, a 2,3-benzodiazepine that selectively blocks ampa receptors was assessed. this selective ampa receptor antagonist potently suppressed 5-ht-induced epscs. since phenethylamine hallucinogens induce head shakes by activating 5-ht2areceptors in the mpfc and this action is modulated by glutamate, we also examined whether selective blockade of ampa receptors would suppress doi-induced head shakes. as predicted, we found that selective blockade of ampa receptors suppressed doi-induced head shakes. given evidence that activation of ampa receptors is an important downstream effect for both channel blocking nmda receptor antagonists and phenethylamine hallucinogens, we also tested multiple doses of doi with a sub-anesthetic dose of mk-801. synergistic action between these two classes of psychotomimetic drugs was demonstrated by mk-801 enhancing doi-induced head shakes and locomotor activity. these findings expand the dependence of both channel blocking nmda receptor antagonists and phenethylamine hallucinogens on enhancing extracellular glutamate. © 2007.”
Xu, Y. Z., & Chen, C.. (2006). Synthesis of deuterium labeled phenethylamine derivatives. Journal of Labelled Compounds and Radiopharmaceuticals
Plain numerical DOI: 10.1002/jlcr.1139
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“The synthesis of a series of five deuterium labeled phenethylamine derivatives, 4-bromo-2,5-[2h6]-dimethoxyphenethylamine (2c-b), 4-chloro-2,5-[2h6]-dimethoxyphenethylamine (2c-c), 2,5-[2h6]-dimethoxy-4-iodophenethylamine (2c-i), 2,5-[2h6]-dimethoxy-4-ethylthiophenethylamine (2c-t-2) and 2,5-[2h6]-dimethoxy-4-n-propylthiophenethylamine (2c-t-7) from 1,4-[2h6]-dimethoxybenzene is described. the isotopically labeled compounds are used as internal standards in gas chromatography-mass spectrometry (gc-ms) assays. copyright © 2006 john wiley & sons, ltd.”
Monte, A. P., Marona-Lewicka, D., Lewis, M. M., Mailman, R. B., Wainscott, D. B., Nelson, D. L., & Nichols, D. E.. (1998). Substituted naphthofurans as hallucinogenic phenethylamine -Ergoline hybrid molecules with unexpected muscarinic antagonist activity. Journal of Medicinal Chemistry
Plain numerical DOI: 10.1021/jm980076u
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“A series of substituted racemic naphthofurans were synthesized as ?hybrid? molecules of the two major prototypical hallucinogenic drug classes, the phenethylamines and the tryptamines/ergolines. although it was hypothesized that these new agents might possess high affinity for the serotonin 5-ht2a/2c receptor subtypes, unexpected affinity for muscarinic receptors was observed. the compounds initially synthesized for this study were (±)-anti- and syn-4-amino-6-methoxy-2a,3,4,5-tetrahydro-2h-naphtho[1,8-bc]furan (4a,b), respectively, and their 8-bromo derivatives 4c,d, respectively. the brominated primary amines 4c,d were assayed initially for activity in the two-lever drug discrimination (dd) paradigm in rats trained to discriminate saline from lsd tartrate (0.08 mg/kg). also, 4c,d were evaluated for their ability to compete against agonist and antagonist radioligands at cloned human 5-ht2a, 5-ht2b, and 5-ht2c receptors. after the syn diastereomers were found to have the highest activity in these preliminary assays, the n-alkylated analogues syn-n,n-dimethyl-4-amino-6-methoxy-2a,3,4,5-tetrahydro-2h-naphtho[1,8-bc]furan (4e) and syn-n,n-dipropyl-4-amino-6-methoxy-2a,3,4,5-tetrahydro-2h-naphtho[1,8-bc]furan (4f) were prepared and assayed for their affinities at [3h]ketanserin-labeled 5-ht2a and [3h]-8-oh-dpat-labeled 5-ht1a sites. all of the molecules tested had relatively low affinity for serotonin receptors, yet a preliminary screen indicated that compound 4d had affinity for muscarinic receptors. thus, 4b,d,e were evaluated for their affinity at muscarinic m1?m5 receptors and also assessed for their functional characteristics at the m1 and m2 isoforms. compound 4d had affinities of 12?33 nm at all of the muscarinic sites, with 4b,e having much lower affinity. all three compounds fully antagonized the effects of carbachol at the m1 receptor, while only 4d completely antagonized carbachol at the m2 receptor. the fact that the naphthofurans lack lsd-like activity suggests that they do not bind to the serotonin receptor in a way such that the tricyclic naphthofuran nucleus is bioisosteric with, and directly superimposable upon, the a, b, and c rings of lsd. this also implies, therefore, that the hallucinogenic phenethylamines cannot be directly superimposed on lsd in a common binding orientation for these two chemical classes, contrary to previous hypotheses.”
Dean, B. V., Stellpflug, S. J., Burnett, A. M., & Engebretsen, K. M.. (2013). 2C or Not 2C: Phenethylamine Designer Drug Review. Journal of Medical Toxicology
Plain numerical DOI: 10.1007/s13181-013-0295-x
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“New groups of synthetic ‘designer drugs’ have increased in popularity over the past several years. these products mimic the euphoric effects of other well-known illicit drugs but are advertised as ‘legal’ highs and are sold over the internet, at raves and night clubs, and in head shops. the 2c series drugs are ring-substituted phenethylamines that belong to a group of designer agents similar in structure to 3,4-methylenedioxy-n-methylamphetamine (mdma, ecstasy). understanding the pharmacology and toxicology of these agents is essential in order to provide the best medical care for these patients. this review focuses on the pharmacology, pharmacokinetics, clinical effects, and treatment of 2c drug intoxication based on available published literature. multiple names under which 2c drugs are sold were identified and tabulated. common features identified in patients intoxicated with 2cs included hallucinations, agitation, aggression, violence, dysphoria, hypertension, tachycardia, seizures, and hyperthermia. patients may exhibit sympathomimetic symptoms or symptoms consistent with serotonin toxicity, but an excited delirium presentation seems to be consistent amongst deaths attributed to 2c drugs; at least five deaths have been reported in the literature in patients intoxicated with 2c drugs. 2c drugs are a group of designer intoxicants, many of which are marketed as legal, but may carry risks that consumers are unaware of. these drugs may be characterized by either serotonergic toxicity or a sympathomimetic toxidrome, but a presentation consistent with excited delirium is consistent amongst the reported 2c-related deaths. treatment of 2c intoxication is primarily supportive, but immediate action is required in the context of excited delirium, hyperthermia, and seizure activity.”
Fantegrossi, W. E., Murnane, K. S., & Reissig, C. J.. (2008). The behavioral pharmacology of hallucinogens. Biochemical Pharmacology
Plain numerical DOI: 10.1016/j.bcp.2007.07.018
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“Until very recently, comparatively few scientists were studying hallucinogenic drugs. nevertheless, selective antagonists are available for relevant serotonergic receptors, the majority of which have now been cloned, allowing for reasonably thorough pharmacological investigation. animal models sensitive to the behavioral effects of the hallucinogens have been established and exploited. sophisticated genetic techniques have enabled the development of mutant mice, which have proven useful in the study of hallucinogens. the capacity to study post-receptor signaling events has lead to the proposal of a plausible mechanism of action for these compounds. the tools currently available to study the hallucinogens are thus more plentiful and scientifically advanced than were those accessible to earlier researchers studying the opioids, benzodiazepines, cholinergics, or other centrally active compounds. the behavioral pharmacology of phenethylamine, tryptamine, and ergoline hallucinogens are described in this review, paying particular attention to important structure activity relationships which have emerged, receptors involved in their various actions, effects on conditioned and unconditioned behaviors, and in some cases, human psychopharmacology. as clinical interest in the therapeutic potential of these compounds is once again beginning to emerge, it is important to recognize the wealth of data derived from controlled preclinical studies on these compounds. © 2007 elsevier inc. all rights reserved.”
Frison, G., Favretto, D., Zancanaro, F., Fazzin, G., & Ferrara, S. D.. (2008). A case of β-carboline alkaloid intoxication following ingestion of Peganum harmala seed extract. Forensic Science International, 179(2–3)
Plain numerical DOI: 10.1016/j.forsciint.2008.05.003
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“β-carboline alkaloids harmine, harmaline, and tetrahydroharmine can stimulate the central nervous system by inhibiting the metabolism of amine neurotransmitters, or by direct interaction with specific receptors; they are found in numerous plants, including peganum harmala, passiflora incarnata and banisteriopsis caapi, and in the entheogen preparation ayahuasca, which is traditionally brewed using b. caapi to enhance the activity of amine hallucinogenic drugs. the ingestion of plant preparations containing β-carboline alkaloids may result in toxic effects, namely visual and auditory hallucinations, locomotor ataxia, nausea, vomiting, confusion and agitation. we report a case of intoxication following intentional ingestion of p. harmala seed infusion; p. harmala seeds were bought over the internet. the harmala alkaloids were identified by gas chromatography-mass spectrometry in the seed extract and the patient’s urine. this is, to our knowledge, the first case of p. harmala intoxication corroborated by toxicological findings. © 2008 elsevier ireland ltd. all rights reserved.”
Nichols, D. E.. (
1998).
The Medicinal Chemistry of Phenethylamine Psychedelics. In The Heffter Review of Psychedelic Research
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“Introduction: this systematic literature review aims to identify documented impacts that windstorms have on human health. windstorms occur frequently and some researchers have predicted an increase in severe gales in the future, resulting in an urgent need to understand the related patterns of morbidity and mortality. study design: systematic literature review. methods: a systematic literature review of international evidence on the impacts of windstorms on human health was conducted in may 2012. results: this review of published evidence demonstrates that human health can be severely affected by windstorms. direct effects occur during the impact phase of a storm, causing death and injury due to the force of the wind. becoming airborne, being struck by flying debris or failing trees and road traffic accidents are the main dangers. indirect effects, occurring during the pre- and post-impact phases of the storm, include fails, lacerations and puncture wounds, and occur when preparing for, or cleaning up after a storm. power outages are a key issue and can lead to electrocution, fires and burns and carbon monoxide poisoning from gasoline powered electrical generators. additionally, worsening of chronic illnesses due to lack of access to medical care or medication can occur. other health impacts include infections and insect bites. conclusion: public health advice can reduce morbidity and mortality from windstorms. findings from this review will provide material for increased awareness and education amongst the public and healthcare professionals to prevent and prepare for these health impacts. nevertheless, more research is needed to identify more specific patterns of health impacts and how these could be reduced in the future. [abstract from author]”
Halberstadt, A. L., & Geyer, M. A.. (2014). Effects of the hallucinogen 2,5-dimethoxy-4-iodophenethylamine (2C-I) and superpotent N-benzyl derivatives on the head twitch response. Neuropharmacology
Plain numerical DOI: 10.1016/j.neuropharm.2013.08.025
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“N-benzyl substitution markedly enhances the affinity of phenethylamine hallucinogens at the 5-ht2areceptor. n-benzyl substituted derivatives of 2,5-dimethoxy-4-iodophenethylamine (2c-i), such as n-(2-methoxybenzyl)-2,5-dimethoxy-4-iodophenethylamine (25i-nbome) and n-(2,3-methylenedioxybenzyl)-2,5-dimethoxy-4-iodophenethylamine (25i-nbmd), have appeared recently as designer drugs, but have not been characterized behaviorally. the head twitch response (htr) is induced by 5-ht2areceptor activation in rats and mice, and is widely used as a behavioral proxy for hallucinogen effects in humans. nevertheless, it is not clear whether phenethylamine hallucinogens reliably provoke this behavior. hence, we investigated whether 2c-i, 25i-nbome and 25i-nbmd induce head twitches in c57bl/6j mice. the htr was assessed using a head-mounted magnet and a magnetometer coil. 2c-i (1-10 mg/kg sc), 25i-nbome (0.1-1 mg/kg sc), and 25i-nbmd (1-10 mg/kg sc) induced the htr. 25i-nbome displayed 14-fold higher potency than 2c-i, and the selective 5-ht2aantagonist m100,907 completely blocked the htr induced by all three compounds. these findings show that phenethylamine hallucinogens induce the htr by activating 5-ht2areceptors. our results demonstrate that 25i-nbome is a highly potent derivative of 2c-i, confirming previous in vitro findings that n-benzyl substitution increases 5-ht2aaffinity. given the high potency and ease of synthesis of n-benzylphenethylamines, it is likely that the recreational use of these hallucinogens will become more widespread in the future. © 2013 elsevier ltd. all rights reserved.”
Roberts, T. B.. (
2006).
Chemical Input, Religious Output–Entheogens: A Pharmatheology Sampler..
Where God and Science Meet: How Brain and Evolutionary Studies Alter Our Understanding of Religion (Vol 3): The Psychology of Religious Experience.
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“(From the chapter) this chapter collects some specimens of pharmatheology and considers the explosive effects entheogens are having on our ideas about religion, including–but not limited to–brain-religion studies. the chapter describes entheogen-derived ideas from some of the major scholars in the field and some of my own leanings on these topics. the expanding interest in entheogens is embedded in the larger intellectual context of multistate mind-body studies. entheogens recast existing questions for churches and society while giving birth to entirely new ones. the chapter raises over 150 questions that deserve to become part of a program of sustained, systematic entheogenic inquiry into religion. (psycinfo database record (c) 2015 apa, all rights reserved)”
Moya, P. R., Berg, K. A., Gutierrez-Hernandez, M. A., Saez-Briones, P., Reyes-Parada, M., Cassels, B. K., & Clarke, W. P.. (2007). Functional Selectivity of Hallucinogenic Phenethylamine and Phenylisopropylamine Derivatives at Human 5-Hydroxytryptamine (5-HT)2A and 5-HT2C Receptors. Journal of Pharmacology and Experimental Therapeutics
Plain numerical DOI: 10.1124/jpet.106.117507
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“2,5-dimethoxy-4-substituted phenylisopropylamines and phenethylamines are 5-hydroxytryptamine (serotonin) (5-ht)2a/2c agonists. the former are partial to full agonists, whereas the latter are partial to weak agonists. however, most data come from studies analyzing phospholipase c (plc)-mediated responses, although additional effectors [e.g., phospholipase a2 (pla2)] are associated with these receptors. we compared two homologous series of phenylisopropylamines and phenethylamines measuring both pla2 and plc responses in chinese hamster ovary-k1 cells expressing human 5-ht2a or 5-ht2c receptors. in addition, we assayed both groups of compounds as head shake inducers in rats. at the 5-ht2c receptor, most compounds were partial agonists for both pathways. relative efficacy of some phenylisopropylamines was higher for both responses compared with their phenethylamine counterparts, whereas for others, no differences were found. at the 5-ht2a receptor, most compounds behaved as partial agonists, but unlike findings at 5-ht2c receptors, all phenylisopropylamines were more efficacious than their phenethylamine counterparts. 2,5-dimethoxyphenylisopropylamine activated only the plc pathway at both receptor subtypes, 2,5-dimethoxyphenethylamine was selective for plc at the 5-ht2c receptor, and 2,5-dimethoxy-4-nitrophenethylamine was pla2-specific at the 5-ht2a receptor. for both receptors, the rank order of efficacy of compounds differed depending upon which response was measured. the phenylisopropylamines were strong head shake inducers, whereas their phenethylamine congeners were not, in agreement with in vitro results and the involvement of 5-ht2a receptors in the head shake response. our results support the concept of functional selectivity and indicate that subtle changes in ligand structure can result in significant differences in the cellular signaling profile.”