1. Academic Validation
  2. 5-HT(3) receptors

5-HT(3) receptors

  • J Biol Chem. 2012 Nov 23;287(48):40239-45. doi: 10.1074/jbc.R112.406496.
Sarah C R Lummis 1
Affiliations

Affiliation

  • 1 Department of Biochemistry, University of Cambridge, Cambridge CB2 1QW, UK. [email protected]
Abstract

5-Hydroxytryptamine type 3 (5-HT(3)) receptors are cation-selective Cys loop receptors found in both the central and peripheral nervous systems. There are five 5-HT(3) receptor subunits (A-E), and all functional receptors require at least one A subunit. Regions from noncontiguous parts of the subunit sequence contribute to the agonist-binding site, and the roles of a range of amino acid residues that form the binding pocket have been identified. Drugs that selectively antagonize 5-HT(3) receptors (the "setrons") are the current gold standard for treatment of chemotherapy-induced and postoperative nausea and vomiting and have potential for the treatment of a range of Other conditions.

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