期刊
PHARMACOLOGY & THERAPEUTICS
卷 130, 期 3, 页码 338-347出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.pharmthera.2011.02.003
关键词
5-Hydroxytryptamine(3); 5-HT; Serotonin; Antagonist; Nausea and vomiting; Irritable bowel syndrome
资金
- NIAAA NIH HHS [R01 AA012643-01A1] Funding Source: Medline
- NINDS NIH HHS [R01 NS043438-01A1] Funding Source: Medline
The 5-Hydroxytryptamine(3) (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 Ca2+, 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. (C) 2011 Elsevier Inc. All rights reserved.
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