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CNS Stimulants: Psychedelic Agents01:22

CNS Stimulants: Psychedelic Agents

Hallucinogens, also known as psychedelic drugs, are a class of substances known for their ability to alter perception, cognition, and emotions. Despite their profound effects on the mind, these drugs are non-addictive, setting them apart from many other abused substances. The mechanism of action of these drugs lies in their impact on the 5-HT2A receptor in the brain. Upon activation, this receptor couples to Gq-type G proteins, triggering a cascade that releases intracellular calcium. This...
Hallucinogens and Psychedelics01:27

Hallucinogens and Psychedelics

Hallucinogens are psychoactive substances that profoundly alter perceptual experiences, generating unreal visual and sensory images. Often referred to as psychedelic drugs — a term derived from the Greek words "psyche" (mind) and "delos" (revealing) — these substances include marijuana and lysergic acid diethylamide (LSD), among others. These drugs vary in intensity and effects.
Marijuana, derived from the dried leaves and flowers of the hemp plant, contains delta-9-tetrahydrocannabinol (THC)...
An Overview of Psychoactive Drugs01:28

An Overview of Psychoactive Drugs

Psychoactive drugs impact brain function, influencing perception, mood, consciousness, cognition, and behavior. These substances are grouped based on their effects and the mechanisms by which they act.
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...
Altered States of Awareness01:06

Altered States of Awareness

Altered states of consciousness represent significant deviations from one's normal mental state. These deviations can range from subtle changes in awareness to profound transformations in perception, thought processes, and sensory experiences. Altered states of consciousness can be triggered by various factors, including drug use, meditation, hypnosis, illness, or even intense fatigue.
The ingestion of substances like stimulants or hallucinogens leads to chemical alterations in the brain that...
Opioid Receptors: Overview01:22

Opioid Receptors: Overview

Opioid receptors, including the mu (μ, MOR), delta (δ, DOR), and kappa (κ, KOR) types, belong to the rhodopsin family of G protein-coupled receptors. These receptors are located throughout the central and peripheral nervous systems and in non-neuronal tissues such as macrophages and astrocytes. Opioid receptor ligands can be categorized into agonists or antagonists. Highly selective agonists include [d-Ala2, MePhe4, Gly(ol)5]-enkephalin or DAMGO for MOR, [D-Pen2, D-Pen5]-enkephalin or DPDPE for...
Introduction to Special Senses01:26

Introduction to Special Senses

Sensory receptors play an integral part in comprehending our external and internal environments. They receive diverse stimuli, converting them into the nervous system's electrochemical signals. This conversion occurs as the stimulus alters the sensory neuron's cell membrane potential, instigating the generation of an action potential. This action potential is subsequently transmitted to the central nervous system (CNS), which integrates with other sensory data or higher cognitive functions.

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Related Experiment Video

Updated: Jun 16, 2026

HSV-Mediated Transgene Expression of Chimeric Constructs to Study Behavioral Function of GPCR Heteromers in Mice
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HSV-Mediated Transgene Expression of Chimeric Constructs to Study Behavioral Function of GPCR Heteromers in Mice

Published on: July 9, 2016

Psychedelics and the human receptorome.

Thomas S Ray1

  • 1Department of Zoology, University of Oklahoma, Norman, Oklahoma, United States of America. tray@ou.edu

Plos One
|February 4, 2010
PubMed
Summary
This summary is machine-generated.

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.

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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.