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.
Original language | English |
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Pages (from-to) | 1228-1238 |
Number of pages | 11 |
Journal | British Journal of Pharmacology |
Volume | 169 |
Issue number | 6 |
Early online date | 17 Apr 2013 |
DOIs | |
Publication status | Published - Jul 2013 |
Bibliographical note
© 2013 The British Pharmacological Society.Keywords
- 5‐HT3 receptor
- ligand‐gated ion channel
- allosteric modulation