Current Pharmaceutical Design

William A. Banks  
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5-HT3 Receptors

Author(s): A. J. Thompson, S. C. R. Lummis.

Abstract:

The 5-HT3 receptor is a member of the Cys-loop family of ligand-gated ion channels. These receptors are located in both the peripheral and central nervous systems, where functional receptors are constructed from five subunits. These subunits may be the same (homopentameric 5-HT3A receptors) or different (heteropentameric receptors, usually comprising of 5-HT3A and 5-HT3B receptor subunits), with the latter having a number of distinct properties. The 5-HT3 receptor binding site is comprised of six loops from two adjacent subunits, and critical ligand binding amino acids in these loops have been largely identified. There are a range of selective agonists and antagonists for these receptors and the pharmacophore is reasonably well understood. There are also a wide range of compounds that can modulate receptor activity. Studies have suggested many diverse potential disease targets that might be amenable to alleviation by 5-HT3 receptor selective compounds but to date only two applications have been fully realised in the clinic: the treatment of emesis and irritable-bowel syndrome.

Keywords: Serotonin receptor, ligand-gated ion channel, 5-HT3 receptor, ligand binding, antagonist, agonist, pharmacology, disease

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Article Details

VOLUME: 12
ISSUE: 28
Year: 2006
Page: [3615 - 3630]
Pages: 16
DOI: 10.2174/138161206778522029
Price: $58