Discriminating between 5‐HT3A and 5‐HT3AB receptors. (27th May 2013)

• Record Type: Journal Article
• Authors: Thompson, AJ; Lummis, SCR
• Is Part Of: British journal of pharmacology. Volume 169:Number 4(2013:Jun.)
• Page Start: 736
• Page End: 747
• Publication Date: 2013-05-27
• Subjects: Pharmacology -- Periodicals; Chemotherapy -- Periodicals; Drug Therapy -- Periodicals; Pharmacology -- Periodicals; 615.1
• DOI: 10.1111/bph.12166
• Languages: English
• ISSNs: 0007-1188

Abstract

<abstract abstract-type="main"> <title> <x xml:space="preserve">Abstract</x> </title> <p>The 5‐HT3B subunit was first cloned in 1999, and co‐expression with the 5‐HT3A subunit results in heteromeric 5‐HT₃AB receptors that are functionally distinct from homomeric 5‐HT₃A receptors. The affinities of competitive ligands at the two receptor subtypes are usually similar, but those of non‐competitive antagonists that bind in the pore often differ. A competitive ligand and allosteric modulator that distinguishes 5‐HT₃A from 5‐HT₃AB receptors has recently been described, and the number of non‐competitive antagonists identified with this ability has increased in recent years. In this review, we discuss the differences between 5‐HT₃A and 5‐HT₃AB receptors and describe the possible sites of action of compounds that can distinguish between them.</p> </abstract>