5-HT2 receptors

Curr Drug Targets CNS Neurol Disord. 2004 Feb;3(1):11-26. doi: 10.2174/1568007043482598.

Abstract

5-HT(2) receptors are G-protein coupled receptors that currently comprise three subtypes: 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. The subtypes are related in their molecular structure, amino acid sequence and signaling properties. 5-HT(2A) and 5-HT(2C) receptors have a widespread distribution and function in the central nervous system. 5-HT(2A)and 5-HT(2C) receptor antagonism is a property of certain antipsychotic and antidepressant drugs. 5-HT(2B) receptors have a restricted expression in the central nervous system. They have an important role in embryogenesis and in the periphery. In this article, selected aspects of 5-HT(2) receptor research are reviewed for each subtype under three main headings : (i) genes, protein structure and receptor signaling; (ii) receptor localization with emphasis on the CNS and (iii) compounds. The general discussion reflects on the reasons for the limited success in the clinic of 5-HT(2) receptor subtype selective drugs.

Publication types

  • Review

MeSH terms

  • Animals
  • Brain / drug effects
  • Brain / metabolism
  • Cloning, Molecular
  • Drug Evaluation / methods
  • Humans
  • Immunohistochemistry
  • Mice
  • Neurons / drug effects
  • Neurons / metabolism*
  • Rats
  • Receptors, Serotonin, 5-HT2 / classification*
  • Receptors, Serotonin, 5-HT2 / drug effects*
  • Receptors, Serotonin, 5-HT2 / genetics
  • Receptors, Serotonin, 5-HT2 / metabolism
  • Selective Serotonin Reuptake Inhibitors / pharmacology
  • Serotonin Antagonists / pharmacology*
  • Serotonin Receptor Agonists / pharmacology*
  • Signal Transduction
  • Structure-Activity Relationship
  • Tissue Distribution

Substances

  • Receptors, Serotonin, 5-HT2
  • Serotonin Antagonists
  • Serotonin Receptor Agonists
  • Serotonin Uptake Inhibitors