Related Experiment Video
Updated: Jul 23, 2026

Quantifying Agonist Activity at G Protein-coupled Receptors
Published on: December 26, 2011
5-HT(3) receptor antagonists
1PRPN CNS, F. Hoffmann-La Roche, 4070 Basel, Switzerland. guy_a.higgins@roche.com
Abstract:
The 5-HT(3) receptor is a ligand-gated ion channel widely distributed in the central and peripheral nervous systems. Many selective 5-HT(3) receptor antagonists have been developed; animal studies with such compounds suggested their potential therapeutic value in combating emesis and a wide range of CNS diseases including anxiety, schizophrenia, drug dependence and Alzheimer's disease. Their successful introduction as anti-emetics, with irritable bowel syndrome emerging as a further indication have partially fulfilled this initial promise. However, the CNS area has been less productive and, to date, no selective 5-HT(3) receptor antagonist has been approved for use in a CNS disease.
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