Correction: Psychedelics and the Human Receptorome
PLoS One March 4, 2010 correction DOI: 10.1371/annotation/e580a864-cf13-40c2-9bd9-b9687a6f0fe4 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Reference work with new experimental data and literature review Qualitative |
|---|---|
| Keywords | Receptor Agonism Pharmacology |
| Citations | 57 |
| Key findings | Psychedelic drugs, especially phenylalkylamines, are not as selective as generally believed, interacting with 42 of 49 broadly assayed sites, and their diverse receptor interaction patterns may underlie qualitative differences in their effects. |
Abstract
We currently understand the mental effects of psychedelics to be caused by agonism or partial agonism of 5-HT 2A (and possibly 5-HT 2C ) receptors, and we understand that psychedelic drugs, especially phenylalkylamines, are fairly selective for these two receptors.This manuscript is a reference work on the receptor affinity pharmacology of psychedelic drugs.New data is presented on the affinity of twenty-five psychedelic drugs at fifty-one receptors, transporters, and ion channels, assayed by the National Institute of Mental Health -Psychoactive Drug Screening Program (NIMH-PDSP).In addition, comparable data gathered from the literature on ten additional drugs is also presented (mostly assayed by the NIMH-PDSP).A new method is introduced for normalizing affinity (K i ) data that factors out potency so that the multi-receptor affinity profiles of different drugs can be directly compared and contrasted.The method is then used to compare the thirty-five drugs in graphical and tabular form.It is shown that psychedelic drugs, especially phenylalkylamines, are not as selective as generally believed, interacting with forty-two of forty-nine broadly assayed sites.The thirty-five drugs of the study have very diverse patterns of interaction with different classes of receptors, emphasizing eighteen different receptors.This diversity of receptor interaction may underlie the qualitative diversity of these drugs.It should be possible to use this diverse set of drugs as probes into the roles played by the various receptor systems in the human mind.
Citations in the library
Cited by 50
- Correlation between the potency of hallucinogens in the mouse head-twitch response assay and their behavioral and subjective effects in other species. Neuropharmacology May 1, 2020
- Psychedelics in Psychiatry: Neuroplastic, Immunomodulatory, and Neurotransmitter Mechanisms Pharmacological Reviews December 16, 2020
- Exploratory study of the dose-related safety, tolerability, and efficacy of dimethyltryptamine (DMT) in healthy volunteers and major depressive disorder. Neuropsychopharmacology September 1, 2022
- Metabolic engineering of Saccharomyces cerevisiae for the de novo production of psilocybin and related tryptamine derivatives Metabolic Engineering March 26, 2020
- Receptor-Enriched Analysis of functional connectivity by targets (REACT): A novel, multimodal analytical approach informed by PET to study the pharmacodynamic response of the brain under MDMA Neuroimage April 4, 2019
and 45 more in the library
Cites 4
- Evidence for 5-HT2 involvement in the mechanism of action of hallucinogenic agents. Life Sciences December 17, 1984
- Differences Between the Mechanism of Action of MDMA, MBDB, and the Classic Hallucinogens. Identification of a New Therapeutic Class: Entactogens Journal of Psychoactive Drugs October 1, 1986
- Effect of Ring Fluorination on the Pharmacology of Hallucinogenic Tryptamines Journal of Medicinal Chemistry October 19, 2000
- Antagonism of the effects of the hallucinogen DOM and the purported 5-HT agonist quipazine by 5-HT2 antagonists. European Journal of Pharmacology July 1, 1983