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.
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Authors | Tina K Machu |
Journal | Pharmacology & therapeutics
(Pharmacol Ther)
Vol. 130
Issue 3
Pg. 338-47
(Jun 2011)
ISSN: 1879-016X [Electronic] England |
PMID | 21356241
(Publication Type: Journal Article, Review)
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Copyright | Copyright © 2011 Elsevier Inc. All rights reserved. |
Chemical References |
- Receptors, Serotonin, 5-HT3
- Serotonin 5-HT3 Receptor Antagonists
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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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