Indoleamine and the phenethylamine hallucinogens: mechanisms of psychotomimetic action
Gerard J. Marek, George K. Aghajanian
Drug and Alcohol Dependence June 1, 1998 DOI: 10.1016/s0376-8716(98)00076-3 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Review Peer reviewed |
|---|---|
| Topics | Mescaline Psilocybin |
| Keywords | Psychotomimetic Hallucinogen Phenethylamine Action physics Pharmacology Biochemistry |
| Citations | 39 |
| Key findings | Indoleamine and phenethylamine hallucinogens bind to the 5-HT2A serotonin receptor, and activation of this receptor mediates their psychotomimetic effects. |
Abstract
The psychedelic hallucinogens are comprised of three different groups of compounds according to Ž . Ž . their chemical structure Fig. 1 : 1 the ergolines Ž which contain an indole moiety e.g. lysergic acid . Ž . diethylamide, LSD ; 2 simple indoleamine hallucinoŽ gens e.g. N,N-dimethyltryptamine, DMT and psilocy. bin which share an indoleamine structure with the Ž endogenous neurotransmitter 5-hydroxytryptamine 5. Ž . HT, serotonin ; and 3 the ring-substituted phenethŽ . ylamine hallucinogens e.g. mescaline . One of the outstanding features of ergoline, indoleamine, and phenethylamine hallucinogens is that they alter all cortical functions including cognition, perception, and mood. This implies that the sites mediating the psychotomimetic effects of these hallucinogens are located in the neocortex or in subcortical areas with efferent projections throughout the neocortex. This review will consider evidence suggesting that both the indoleamine and phenethylamine hallucinogens bind to a common neurotransmitter receptor in the brain, Ž . the 5-hydroxytryptamine 5-HT receptor, and 2A 2A that subsequent activation of this serotonin receptor mediates the psychotomimetic effects of these halluciŽ . nogens. We will also discuss potential site s in the brain at which the hallucinogens exert their psychotomimetic effects.
Comparable studies
Other narrative reviews on mescaline, most cited first.
| Study | Year | Design | Participants |
|---|---|---|---|
| Study of a New Schizophrenomimetic Drug—Sernyl | 1959 | Review | |
| Hallucinogens and Serotonin 5-HT2A Receptor-Mediated Signaling Pathways | 2017 | Review | |
| Hallucinogens in Mental Health: Preclinical and Clinical Studies on LSD, Psilocybin, MDMA, and Ketamine | 2020 | Review | |
| Legal highs: staying on top of the flood of novel psychoactive substances | 2015 | Review | |
| Psychedelic Drugs in Biomedicine | 2017 | Review |
Citations in the library
Cited by 15
- Amphetamine, 3,4-Methylenedioxymethamphetamine, Lysergic Acid Diethylamide, and Metabolites of the Catecholamine Neurotransmitters Are Agonists of a Rat Trace Amine Receptor Molecular Pharmacology December 1, 2001
- Acute psychological and physiological effects of psilocybin in healthy humans: a double-blind, placebo-controlled dose?effect study Psychopharmacology March 1, 2004
- Subjective effects and tolerability of the South American psychoactive beverage Ayahuasca in healthy volunteers Psychopharmacology February 22, 2001
- Topographic pharmaco‐EEG mapping of the effects of the South American psychoactive beverage ayahuasca in healthy volunteers British Journal of Clinical Pharmacology June 1, 2002
- LSD and DOB: interaction with 5‐HT2A receptors to inhibit NMDA receptor‐mediated transmission in the rat prefrontal cortex European Journal of Neuroscience September 1, 1999
and 10 more in the library
Cites 21
- Subanesthetic Effects of the Noncompetitive NMDA Antagonist, Ketamine, in Humans Archives of General Psychiatry March 1, 1994
- Evidence for 5-HT2 involvement in the mechanism of action of hallucinogenic agents. Life Sciences December 17, 1984
- 5-HT2AReceptor-Mediated Regulation of Brain-Derived Neurotrophic Factor mRNA in the Hippocampus and the Neocortex Journal of Neuroscience April 15, 1997
- Lysergic Acid Diethylamide: Sensitive Neuronal Units in the Midbrain Raphe Science August 16, 1968
- Mescaline-induced psychopathological, neuropsychological, and neurometabolic effects in normal subjects: experimental psychosis as a tool for psychiatric research. Biological Psychiatry December 1, 1992
and 16 more in the library