5-HT4 receptor - Tanso Biosciences

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... [read more] 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gastro-oesophageal reflux, constipation and constipation-predominant irritable bowel syndrome (IBS-c), before they were withdrawn due to cardiovascular side-effects. [close]


Human	HTR4 5-hydroxytryptamine receptor 4
Mouse	Htr4 5 hydroxytryptamine (serotonin) receptor 4

Human

HTR4

5-hydroxytryptamine receptor 4

Mouse

Htr4

5 hydroxytryptamine (serotonin) receptor 4

Species	Receptor	Family	Assays
Human	HTR4 5-hydroxytryptamine receptor 4	5-Hydroxytryptamine receptors ⋅	Available Assay modes: Agonist ⋅ Inverse agonist ⋅ Antagonist ⋅ PAM ⋅ NAM Panels: Human non-orphan GPCRs ⋅ Safety Premium ⋅ Cardiology ⋅ à la carte	Reference agonist: serotonin EC50: 26 nM
Mouse	Htr4 5 hydroxytryptamine (serotonin) receptor 4	5-Hydroxytryptamine receptors ⋅	Available Assay modes: Agonist ⋅ Inverse agonist ⋅ Antagonist ⋅ PAM ⋅ NAM Panels: Mouse non-orphan GPCRs ⋅ à la carte	Reference agonist: serotonin EC50: 24 nM

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