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gastro-oesophageal reflux, constipation and constipation-predominant irritable bowel syndrome (IBS-c), before they were withdrawn due to cardiovascular side-effects.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
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Human
Available
Assay modes:
Agonist
Inverse agonist
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PAM
NAM
Panels:
Human non-orphan GPCRs
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Cardiology
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Reference agonist:
serotonin
EC50:
26 nM
Mouse
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Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
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Mouse non-orphan GPCRs
à la carte
Reference agonist:
serotonin
EC50:
24 nM