Related Experiment Video
Updated: Jun 11, 2025

HSV-Mediated Transgene Expression of Chimeric Constructs to Study Behavioral Function of GPCR Heteromers in Mice
Published on: July 9, 2016
Chemistry/structural biology of psychedelic drugs and their receptor(s)
Ryan H Gumpper1, David E Nichols1
1Department of Chemical Biology and Medicinal Chemistry, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina, USA.
Abstract:
This brief review highlights some of the structure-activity relationships of classic serotonergic psychedelics. In particular, we discuss structural features of three chemotypes: phenethylamines, ergolines and certain tryptamines, which possess psychedelic activity in humans. Where they are known, we point out the underlying molecular mechanisms utilized by each of the three chemotypes of psychedelic molecules. With a focus on the 5-HT2A receptor subtype, a G-protein coupled receptor known to be the primary target of psychedelics, we refer to several X-ray and cryoEM structures, with a variety of ligands bound, to illustrate the underlying atomistic basis for some of the known pharmacological observations of psychedelic drug actions. LINKED ARTICLES: This article is part of a themed issue Emerging Therapeutic Opportunities for Psychedelic and Related Drugs. To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v183.14/issuetoc.
More Related Videos
18:45Harvesting and Cryo-cooling Crystals of Membrane Proteins Grown in Lipidic Mesophases for Structure Determination by Macromolecular Crystallography
Published on: September 2, 2012
11:24High Precision FRET at Single-molecule Level for Biomolecule Structure Determination
Published on: May 13, 2017
Related Concept Videos
CNS Stimulants: Psychedelic Agents
Hallucinogens and Psychedelics
Marijuana, derived from the dried leaves and flowers of the hemp plant, contains...
An Overview of Psychoactive Drugs
Stimulants such as cocaine, amphetamines, and nicotine enhance brain activity, leading to increased alertness, attention, and energy. These drugs typically raise heart rate, blood pressure, and body temperature. While they can induce feelings of euphoria, their misuse can result in severe health...
Structure-Activity Relationships and Drug Design
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence...
CNS Stimulants: Cocaine, Amphetamines and Cannabinoids
Ligand-Gated Ion Channel Receptor: Gating Mechanism