5-Chloroindole: a potent allosteric modulator of the 5-HT3 receptor: Allosteric modulation of the 5-HT3receptor

Research output: Contribution to journalArticle

Authors

Abstract

The 5-HT3 receptor is a ligand-gated ion channel that is modulated allosterically by various compounds including colchicine, alcohols and volatile anaesthetics. However the positive allosteric modulators (PAMs) identified to date have low affinity, which hinders investigation because of non-selective effects at pharmacologically active concentrations. The present study identifies 5-chloroindole (Cl-indole) as a potent PAM of the 5-HT3 receptor.

Bibliographic note

© 2013 The British Pharmacological Society.

Details

Original languageEnglish
Pages (from-to)1228-1238
Number of pages11
JournalBritish Journal of Pharmacology
Volume169
Issue number6
Early online date17 Apr 2013
Publication statusPublished - Jul 2013

Keywords

  • 5‐HT3 receptor, ligand‐gated ion channel, allosteric modulation