5-HT4 receptor
Overview
The 5-HT4 receptor is a GPCR that couples via Gs to increase cAMP production. The structure displays less than 34% amino acid sequence identity to other 5-HT GPCRs justifying the separate family. At least 10 splice variants have been identified.PharmacologySelective agonists (e.g. RS 67506 [partial agonist]) and antagonists (e.g. SB 204070) are available.Clinical significance5-HT4 receptor agonists (e.g. cisapride, tegaserod) were effective drugs reducing the symptoms of gastro-oesophageal reflux, constipation and constipation-predominant irritable bowel syndrome (IBS-c), before they were withdrawn due to cardiovascular side-effects.Excerpt from IUPHAR/BPS Guide to Pharmacology Filters Sort resultsReset ApplyFilters Sort resultsReset Apply
