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Identification of N,N-dimethyltryptamine and beta-carbolines in psychotropic ayahuasca beverage

May 27, 2008 / Ayahuasca, Biology & Ethnobotany, Papers, Pharmacology & Chemistry, Publications / By / , , , ,

Abstract

Recently many people have shown great interest in traditional indigenous practices and popular medicine, involving the ingestion of natural psychotropic drugs. We received a request to analyze and determine the nature of a dark green liquid with a dark brown plant sediment, which the police had seized at an airport and inside the home of a person belonging to the ‘Santo Daime’ religious movement. Gas chromatography/mass spectrometry analysis of the extract identified N,N-dimethyltryptamine, a potent hallucinogen, and the β-carboline alkaloids harmine and harmaline, revealing monoamine oxidase A-inhibiting properties. These substances are typical components of Ayahuasca, a South American psychotropic beverage obtained by boiling the bark of the liana Banisteriopsis caapi together with the leaves of various admixture plants, principally Psychotria viridis.

Gambelunghe, C., Aroni, K., Rossi, R., Moretti, L., & Bacci, M. (2008). Identification of N, N‐dimethyltryptamine and β‐carbolines in psychotropic ayahuasca beverage. Biomedical Chromatography, 22(10), 1056-1059. 10.1002/bmc.1023
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Selective 5-HT2A agonist hallucinogens: A review of pharmacological interaction and corollary perceptual effects

May 23, 2008 / DMT, LSD, Mushrooms / Psilocybin, Neuroscience, Papers, Psychology, Publications / By /

Abstract

The most potent tryptamine hallucinogens – such as DMT, psilocybin, and LSD – are all active at the 5-HT2A receptor subtype and all produce similar visual perceptual results that are immediately recognizable as uniquely psychedelic. Although it is widely accepted that selective serotonin receptor subtype 2A agonism is directly responsible for producing the distinct hallucinations seen on a psychedelic trip, no single theory has yet explained why this is so. Utilizing what we know about psychedelic tryptamine receptor interaction, sensory processing circuits in the neocortex, and EEG scans of psychedelics in action, this review will propose a novel multi-state theory of psychedelic action which invokes a variety of neural processing mechanisms, including phase-coupled neural oscillators; network excitation, disinhibition, and destabilization; recurrent feedback excitation; and neural circuit spike synchrony and brainwave cohesion to close the knowledge gap between the pharmaceutical interactions of selective 5-HT2A hallucinogens, their direct effects on perception and consciousness at varying dose ranges, and their potential long-term adverse effects.

Kent, J. (2008). Selective 5-HT2A agonist hallucinogens: A review of pharmacological interaction and corollary perceptual effects. Beta Review.

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Effects of varied doses of psilocybin on time interval reproduction in human subjects

April 11, 2008 / Mushrooms / Psilocybin, Papers, Psychology, Publications / By / , , ,

Abstract

Action of a hallucinogenic substance, psilocybin, on internal time representation was investigated in two double-blind, placebo-controlled studies: Experiment 1 with 12 subjects and graded doses, and Experiment 2 with 9 subjects and a very low dose. The task consisted in repeated reproductions of time intervals in the range from 1.5 to 5 s. The effects were assessed by parameter κκ of the ‘dual klepsydra’ model of internal time representation, fitted to individual response data and intra-individually normalized with respect to initial values. The estimates View the MathML sourceκˆ were in the same order of magnitude as in earlier studies. In both experiments, κκ was significantly increased by psilocybin at 90 min from the drug intake, indicating a higher loss rate of the internal duration representation. These findings are tentatively linked to qualitative alterations of subjective time in altered states of consciousness.

Wackermann, J., Wittmann, M., Hasler, F., & Vollenweider, F. X. (2008). Effects of varied doses of psilocybin on time interval reproduction in human subjects. Neuroscience letters, 435(1), 51-55. https://dx.doi.org/10.1016/j.neulet.2008.02.006
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The correlation between ketamine and posttraumatic stress disorder in burned service members

February 22, 2008 / Anxiety Disorders / PTSD, Ketamine, Papers, Psychology, Publications / By / , , , ,

Abstract

BACKGROUND:

Predisposing factors for posttraumatic stress disorder (PTSD) include experiencing a traumatic event, threat of injury or death, and untreated pain. Ketamine, an anesthetic, is used at low doses as part of a multimodal anesthetic regimen. However, since ketamine is associated with psychosomatic effects, there is a concern that ketamine may increase the risk of developing PTSD. This study investigated the prevalence of PTSD in Operation Iraqi Freedom/Operation Enduring Freedom (OIF/OEF) service members who were treated for burns in a military treatment center.

METHODS:

The PTSD Checklist-Military (PCL-M) is a 17-question screening tool for PTSD used by the military. A score of 44 or higher is a positive screen for PTSD. The charts of all OIF/OEF soldiers with burns who completed the PCL-M screening tool (2002-2007) were reviewed to determine the number of surgeries received, the anesthetic regime used, including amounts given, the total body surface area burned, and injury severity score. Morphine equivalent units were calculated using standard dosage conversion factors.

RESULTS:

The prevalence of PTSD in patients receiving ketamine during their operation(s) was compared with patients not receiving ketamine. Of the 25,000 soldiers injured in OIF/OEF, United States Army Institute of Surgical Research received 603 burned casualties, of which 241 completed the PCL-M. Of those, 147 soldiers underwent at least one operation. Among 119 patients who received ketamine during surgery and 28 who did not; the prevalence of PTSD was 27% (32 of 119) versus 46% (13 of 28), respectively (p = 0.044).

CONCLUSIONS:

Contrary to expectations, patients receiving perioperative ketamine had a lower prevalence of PTSD than soldiers receiving no ketamine during their surgeries despite having larger burns, higher injury severity score, undergoing more operations, and spending more time in the ICU.

McGhee, L. L., Maani, C. V., Garza, T. H., Gaylord, K. M., & Black, I. H. (2008). The correlation between ketamine and posttraumatic stress disorder in burned service members. Journal of Trauma and Acute Care Surgery, 64(2), S195-S199. https://dx.doi.org/10.1097/TA.0b013e318160ba1d
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The behavioral pharmacology of hallucinogens

January 1, 2008 / DMT, LSD, MDMA, Mescaline / Cacti, Mushrooms / Psilocybin, Papers, Pharmacology & Chemistry, Publications / By / , ,

Abstract

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.

Fantegrossi, W. E.,  Murnane, K. S., & Reissig, C. J. (2008). The behavioral pharmacology of hallucinogens. Biochemical Pharmacology 75(1), 17–33. http://dx.doi.org/10.1016/j.bcp.2007.07.018
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Comparative potencies of MDMA analogues as inhibitors of [3H]noradrenaline and [3H]5-HT transport in mammalian cell lines

December 1, 2007 / MDMA, Papers, Pharmacology & Chemistry, Publications / By / , , , , ,

Abstract

Background and purpose:Illegal ‘ecstasy’ tablets frequently contain 3,4-methylenedioxymethamphetamine (MDMA)-like compounds of unknown pharmacological activity. Since monoamine transporters are one of the primary targets of MDMA action in the brain, a number of MDMA analogues have been tested for their ability to inhibit [fusion_builder_container hundred_percent=”yes” overflow=”visible”][fusion_builder_row][fusion_builder_column type=”1_1″ background_position=”left top” background_color=”” border_size=”” border_color=”” border_style=”solid” spacing=”yes” background_image=”” background_repeat=”no-repeat” padding=”” margin_top=”0px” margin_bottom=”0px” class=”” id=”” animation_type=”” animation_speed=”0.3″ animation_direction=”left” hide_on_mobile=”no” center_content=”no” min_height=”none”][3H]noradrenaline uptake into rat PC12 cells expressing the noradrenaline transporter (NET) and [3H]5-HT uptake into HEK293 cells stably transfected with the 5-HT transporter (SERT).

Experimental approach:Concentration–response curves for the following compounds at both NET and SERT were determined under saturating substrate conditions: 4-hydroxy-3-methoxyamphetamine (HMA), 4-hydroxy 3-methoxymethamphetamine (HMMA), 3,4-methylenedioxy-N-hydroxyamphetamine (MDOH), 2,5-dimethoxy-4-bromophenylethylamine (2CB), 3,4-dimethoxymethamphetamine (DMMA), 3,4-methylenedioxyphenyl-2-butanamine (BDB), 3,4-methylenedioxyphenyl- N-methyl-2-butanamine (MBDB) and 2,3-methylenedioxymethamphetamine (2,3-MDMA).

Key results: 2,3-MDMA was significantly less potent than MDMA at SERT, but equipotent with MDMA at NET. 2CB and BDB were both significantly less potent than MDMA at NET, but equipotent with MDMA at SERT. MBDB, DMMA, MDOH and the MDMA metabolites HMA and HMMA, were all significantly less potent than MDMA at both NET and SERT.

Conclusions and implications: This study provides an important insight into the structural requirements of MDMA analogue affinity at both NET and SERT. It is anticipated that these results will facilitate understanding of the likely pharmacological actions of structural analogues of MDMA.

Montgomery, T., Buon, C., Eibauer, S., Guiry, P. J., Keenan, A.K., & McBean, G. J. (2007). Comparative potencies of MDMA analogues as inhibitors of [3H]noradrenaline and [3H]5-HT transport in mammalian cell lines. British Journal of Pharmacology, 152(7), 1121–1130. http://dx.doi.org/10.1038/sj.bjp.0707473
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Psilocybin links binocular rivalry switch rate to attention and subjective arousal levels in humans

September 14, 2007 / Mushrooms / Psilocybin, Neuroscience, Papers, Publications / By / , , , , ,

Abstract

Rationale: Binocular rivalry occurs when different images are simultaneously presented to each eye. During continual viewing of this stimulus, the observer will experience repeated switches between visual awareness of the two images. Previous studies have suggested that a slow rate of perceptual switching may be associated with clinical and drug-induced psychosis.

Objectives: The objective of the study was to explore the proposed relationship between binocular rivalry switch rate and subjective changes in psychological state associated with 5-HT2A receptor activation.

Materials and methods: This study used psilocybin, the hallucinogen found naturally in Psilocybe mushrooms that had previously been found to induce psychosis-like symptoms via the 5-HT2A receptor. The effects of psilocybin (215 μg/kg) were considered alone and after pretreatment with the selective 5-HT2A antagonist ketanserin (50 mg) in ten healthy human subjects.

Results: Psilocybin significantly reduced the rate of binocular rivalry switching and increased the proportion of transitional/mixed percept experience. Pretreatment with ketanserin blocked the majority of psilocybin’s “positive” psychosis-like hallucinogenic symptoms. However, ketanserin had no influence on either the psilocybin-induced slowing of binocular rivalry or the drug’s “negative-type symptoms” associated with reduced arousal and vigilance.

Conclusions: Together, these findings link changes in binocular rivalry switching rate to subjective levels of arousal and attention. In addition, it suggests that psilocybin’s effect on binocular rivalry is unlikely to be mediated by the 5-HT2A receptor.

Carter, O. L., Hasler, F., Pettigrew, J. D., Wallis, G. M., Liu, G. B., & Vollenweider, F. X. (2007). Psilocybin links binocular rivalry switch rate to attention and subjective arousal levels in humans. Psychopharmacology, 195(3), 415-424. 10.1007/s00213-007-0930-9

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Effects of ayahuasca on psychometric measures of anxiety, panic-like and hopelessness in Santo Daime members

July 27, 2007 / Anxiety Disorders / PTSD, Ayahuasca, Depressive Disorders, Papers, Psychology, Publications / By / , , , ,

Abstract

The use of the hallucinogenic brew ayahuasca, obtained from infusing the shredded stalk of the malpighiaceous plant Banisteriopsis caapi with the leaves of other plants such as Psychotria viridis, is growing in urban centers of Europe, South and North America in the last several decades. Despite this diffusion, little is known about its effects on emotional states. The present study investigated the effects of ayahuasca on psychometric measures of anxiety, panic-like and hopelessness in members of the Santo Daime, an ayahuasca-using religion. Standard questionnaires were used to evaluate state-anxiety (STAI-state), trait-anxiety (STAI-trait), panic-like (ASI-R) and hopelessness (BHS) in participants that ingested ayahuasca for at least 10 consecutive years. The study was done in the Santo Daime church, where the questionnaires were administered 1 h after the ingestion of the brew, in a double-blind, placebo-controlled procedure. While under the acute effects of ayahuasca, participants scored lower on the scales for panic and hopelessness related states. Ayahuasca ingestion did not modify state- or trait-anxiety. The results are discussed in terms of the possible use of ayahuasca in alleviating signs of hopelessness and panic-like related symptoms.

Santos, R. G., Landeira-Fernandez, J., Strassman, R. J., Motta, V., & Cruz, A. P. M. (2007). Effects of ayahuasca on psychometric measures of anxiety, panic-like and hopelessness in Santo Daime members. Journal of Ethnopharmacology, 112(3), 507-513. http://dx.doi.org/10.1016/j.jep.2007.04.012
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Psilocybin-induced stimulus control in the rat

June 22, 2007 / Mushrooms / Psilocybin, Neuroscience, Papers, Publications / By / , , ,

Abstract

Although psilocybin has been trained in the rat as a discriminative stimulus, little is known of the pharmacological receptors essential for stimulus control. In the present investigation rats were trained with psilocybin and tests were then conducted employing a series of other hallucinogens and presumed antagonists. An intermediate degree of antagonism of psilocybin was observed following treatment with the 5-HT2A receptor antagonist, M100907. In contrast, no significant antagonism was observed following treatment with the 5-HT1A/7 receptor antagonist, WAY-100635, or the DA D2 antagonist, remoxipride. Psilocybin generalized fully to DOM, LSD, psilocin, and, in the presence of WAY-100635, DMT while partial generalization was seen to 2C-T-7 and mescaline. LSD and MDMA partially generalized to psilocybin and these effects were completely blocked by M-100907; no generalization of PCP to psilocybin was seen. The present data suggest that psilocybin induces a compound stimulus in which activity at the 5-HT2A receptor plays a prominent but incomplete role. In addition, psilocybin differs from closely related hallucinogens such as 5-MeO-DMT in that agonism at 5-HT1A receptors appears to play no role in psilocybin-induced stimulus control.

Winter, J. C., Rice, K. C., Amorosi, D. J., & Rabin, R. A. (2007). Psilocybin-induced stimulus control in the rat. Pharmacology Biochemistry and Behavior, 87(4), 472-480. http://dx.doi.org/10.1016/j.pbb.2007.06.003
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Brave New World versus Island — Utopian and Dystopian Views on Psychopharmacology

May 8, 2007 / Papers, Philosophy & Religious Studies, Publications / By /

Abstract

Aldous Huxley’s Brave New World is a famous dystopia, frequently called upon in public discussions about new biotechnology. It is less well known that 30 years later Huxley also wrote a utopian novel, called Island. This paper will discuss both novels focussing especially on the role of psychopharmacological substances. If we see fiction as a way of imagining what the world could look like, then what can we learn from Huxley’s novels about psychopharmacology and how does that relate to the discussion in the ethical and philosophical literature on this subject? The paper argues that in the current ethical discussion the dystopian vision on psychopharmacology is dominant, but that a comparison between Brave New World and Island shows that a more utopian view is possible as well. This is illustrated by a discussion of the issue of psychopharmacology and authenticity. The second part of the paper draws some further conclusions for the ethical debate on psychopharmacology and human enhancement, by comparing the novels not only with each other, but also with our present reality. It is claimed that the debate should not get stuck in an opposition of dystopian and utopian views, but should address important issues that demand attention in our real world: those of evaluation and governance of enhancing psychopharmacological substances in democratic, pluralistic societies.

Schermer, M. H. N. (2007). Brave New World versus Island—Utopian and Dystopian Views on Psychopharmacology. Medicine, Health Care and Philosophy, 10(2), 119-128. https://dx.doi.org/10.1007/s11019-007-9059-1

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