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Psychedelics and the human receptorome
1Department of Zoology, University of Oklahoma, Norman, Oklahoma, United States of America. tray@ou.edu
Plos One
|February 4, 2010
Summary
Psychedelic drugs, particularly phenylalkylamines, interact with more receptors than previously thought. This study reveals diverse receptor binding profiles, suggesting varied mental effects and potential for new research probes.
Area of Science:
- Neuroscience
- Pharmacology
- Psychopharmacology
Background:
- The mental effects of psychedelics are primarily attributed to 5-HT(2A) receptor agonism.
- Psychedelic drugs, especially phenylalkylamines, were believed to be highly selective for 5-HT(2A) and 5-HT(2C) receptors.
Purpose of the Study:
- To provide a comprehensive reference on the receptor affinity pharmacology of psychedelic drugs.
- To present new data on the binding affinities of 35 psychedelic drugs across 51 targets.
- To introduce a novel method for normalizing affinity data to enable direct comparison of multi-receptor profiles.
Main Methods:
- Assay of 25 psychedelic drugs at 51 receptors, transporters, and ion channels via the NIMH-PDSP.
- Inclusion of literature data for 10 additional drugs, also largely from NIMH-PDSP.
- Development and application of a new affinity (K(i)) normalization method factoring out drug potency.
Main Results:
- Psychedelic drugs, including phenylalkylamines, exhibit broader interactions than anticipated, engaging 42 of 49 assayed sites.
- A significant diversity in multi-receptor affinity profiles was observed across the 35 studied drugs.
- Eighteen distinct receptor classes were highlighted as interaction points, indicating complex pharmacology.
Conclusions:
- The common belief in the high selectivity of psychedelic drugs is challenged by new data.
- The diverse receptor interaction patterns of these drugs likely contribute to their varied qualitative effects.
- These findings position psychedelic compounds as valuable tools for investigating the roles of specific receptor systems in the human mind.
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