5-HT(4) receptors: history, molecular pharmacology and brain functions

Neuropharmacology. 2008 Nov;55(6):922-31. doi: 10.1016/j.neuropharm.2008.05.013. Epub 2008 May 23.

Abstract

Twenty years ago, we started the characterization of a 5-HT receptor coupled to cAMP production in neurons. This receptor obviously had a different pharmacology to the other 5-HT receptors described at that time, i.e. the 5-HT(1), 5-HT(2), 5-HT(3) receptors. We proposed to name it the 5-HT(4) receptor. Nowadays, 5-HT(4) receptors are one of the most studied GPCRs belonging to the "rhodopsin" family. Thanks to the existence of a great variety of ligands with inverse agonist, partial agonist, agonist and antagonist profiles, the pharmacological and physiological properties of this receptor are beginning to emerge. Although some 5-HT(4) partial agonists have been on the market for gastro-intestinal pathologies, 5-HT(4) receptor drugs have still to be commercialized for brain disorders. However, since 5-HT(4) receptors have recognized effects on memory, depression and feeding in animal models, there is still hope for a therapeutic destiny of this interesting target in brain disorders.

Publication types

  • Historical Article
  • Review

MeSH terms

  • Animals
  • Brain / drug effects*
  • Brain / physiology*
  • Cyclic AMP / metabolism
  • History, 20th Century
  • History, 21st Century
  • Humans
  • Models, Molecular
  • Receptors, Serotonin* / genetics
  • Receptors, Serotonin* / history
  • Receptors, Serotonin* / metabolism
  • Serotonin Agents / pharmacology*

Substances

  • Receptors, Serotonin
  • Serotonin Agents
  • Cyclic AMP