d-Lysergic Acid Diethylamide (LSD) as a Model of Psychosis: Mechanism of Action and Pharmacology

Int J Mol Sci. 2016 Nov 23;17(11):1953. doi: 10.3390/ijms17111953.

Abstract

d-Lysergic Acid Diethylamide (LSD) is known for its hallucinogenic properties and psychotic-like symptoms, especially at high doses. It is indeed used as a pharmacological model of psychosis in preclinical research. The goal of this review was to understand the mechanism of action of psychotic-like effects of LSD. We searched Pubmed, Web of Science, Scopus, Google Scholar and articles' reference lists for preclinical studies regarding the mechanism of action involved in the psychotic-like effects induced by LSD. LSD's mechanism of action is pleiotropic, primarily mediated by the serotonergic system in the Dorsal Raphe, binding the 5-HT2A receptor as a partial agonist and 5-HT1A as an agonist. LSD also modulates the Ventral Tegmental Area, at higher doses, by stimulating dopamine D₂, Trace Amine Associate receptor 1 (TAAR₁) and 5-HT2A. More studies clarifying the mechanism of action of the psychotic-like symptoms or psychosis induced by LSD in humans are needed. LSD's effects are mediated by a pleiotropic mechanism involving serotonergic, dopaminergic, and glutamatergic neurotransmission. Thus, the LSD-induced psychosis is a useful model to test the therapeutic efficacy of potential novel antipsychotic drugs, particularly drugs with dual serotonergic and dopaminergic (DA) mechanism or acting on TAAR₁ receptors.

Keywords: LSD; TAAR1; atypical antipsychotics; dopamine; hallucinogens; psychosis; serotonin.

Publication types

  • Review

MeSH terms

  • Animals
  • Antipsychotic Agents / pharmacology
  • Behavior, Animal / drug effects
  • Disease Models, Animal
  • Dopamine / metabolism
  • Dopamine / pharmacology
  • Dorsal Raphe Nucleus / drug effects
  • Dorsal Raphe Nucleus / metabolism*
  • Dorsal Raphe Nucleus / physiopathology
  • Drug Evaluation, Preclinical
  • Hallucinogens / metabolism
  • Hallucinogens / pharmacology*
  • Humans
  • Lysergic Acid Diethylamide / metabolism
  • Lysergic Acid Diethylamide / pharmacology*
  • Psychotic Disorders / drug therapy
  • Psychotic Disorders / metabolism*
  • Psychotic Disorders / physiopathology
  • Rats
  • Receptor, Serotonin, 5-HT1A / metabolism
  • Receptor, Serotonin, 5-HT2A / metabolism
  • Receptors, Dopamine / metabolism
  • Receptors, G-Protein-Coupled / metabolism
  • Receptors, Glutamate / metabolism
  • Serotonin Receptor Agonists / metabolism
  • Serotonin Receptor Agonists / pharmacology*
  • Synaptic Transmission / drug effects
  • Ventral Tegmental Area / drug effects
  • Ventral Tegmental Area / metabolism*
  • Ventral Tegmental Area / physiopathology

Substances

  • Antipsychotic Agents
  • Hallucinogens
  • Receptor, Serotonin, 5-HT2A
  • Receptors, Dopamine
  • Receptors, G-Protein-Coupled
  • Receptors, Glutamate
  • Serotonin Receptor Agonists
  • Receptor, Serotonin, 5-HT1A
  • Lysergic Acid Diethylamide
  • Dopamine
  • Trace amine-associated receptor 1