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Therapeutics of 5-HT3 receptor antagonists: current uses and future directions.

Abstract
The 5-Hydroxytryptamine3 (5-HT3) receptor is a member of the cys-loop family of ligand gated ion channels, of which the nicotinic acetylcholine receptor is the prototype. All other 5-HT receptors identified to date are metabotropic receptors. The 5-HT3 receptor is present in the central and peripheral nervous systems, as well as a number of non-nervous tissues. As an ion channel that is permeable to the cations, Na(+), K(+), and Ca(2+), the 5-HT3 receptor mediates fast depolarizing responses in pre- and post-synaptic neurons. As such, 5-HT3 receptor antagonists that are used clinically block afferent and efferent synaptic transmission. The most well established physiological roles of the 5-HT3 receptor are to coordinate emesis and regulate gastrointestinal motility. Currently marketed 5-HT3 receptor antagonists are indicated for the treatment of chemotherapy, radiation, and anesthesia-induced nausea and vomiting, as well as irritable bowel syndrome. Other therapeutic uses that have been explored include pain and drug addiction. The 5-HT3 receptor is one of a number of receptors that play a role in mediating nausea and vomiting, and as such, 5-HT3 receptor antagonists demonstrate the greatest anti-emetic efficacy when administered in combination with other drug classes.
AuthorsTina K Machu
JournalPharmacology & therapeutics (Pharmacol Ther) Vol. 130 Issue 3 Pg. 338-47 (Jun 2011) ISSN: 1879-016X [Electronic] England
PMID21356241 (Publication Type: Journal Article, Review)
CopyrightCopyright © 2011 Elsevier Inc. All rights reserved.
Chemical References
  • Receptors, Serotonin, 5-HT3
  • Serotonin 5-HT3 Receptor Antagonists
Topics
  • Animals
  • Forecasting
  • Gastrointestinal Motility (drug effects, physiology)
  • Humans
  • Irritable Bowel Syndrome (drug therapy, metabolism)
  • Nausea (drug therapy, metabolism)
  • Receptors, Serotonin, 5-HT3 (metabolism)
  • Serotonin 5-HT3 Receptor Antagonists (pharmacology, therapeutic use)
  • Vomiting (drug therapy, metabolism)

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