5-HT3 Receptors

5-Hydroxytryptamine type 3 (5-HT3) receptors are cation-selective Cys loop receptors found in both the central and peripheral nervous systems. There are five 5-HT3 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-HT3 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.