- Nomenclature
- 5-hydroxytryptamine receptor 4
- Available assay modes
- Agonist, Inverse agonist, Antagonist, PAM, NAM
- Panels
- à la carte, Cardiology, Human non-orphan GPCRs
5-Hydroxytryptamine receptors
5-HT receptors are, with the exception of the ionotropic 5-HT3 class, GPCRs where the endogenous agonist is 5-hydroxytryptamine. The diversity of metabotropic 5-HT receptors is increased by alternative splicing that produces isoforms of the 5-HT2A (non-functional), 5-HT2C (non-functional), 5-HT4, 5-HT6 (non-functional) and 5-HT7 receptors. Unique amongst the GPCRs, RNA editing produces 5-HT2C receptor isoforms that differ in function, such as efficiency and specificity of coupling to Gq/11 and also pharmacology [1,2]. Most 5-HT receptors (except 5-ht1e and 5-ht5b) play specific roles mediating functional responses in different tissues (reviewed by [3,4]).References
- Bockaert J, Claeysen S, Bécamel C, et al. Neuronal 5-HT metabotropic receptors: fine-tuning of their structure, signaling, and roles in synaptic modulation. Cell Tissue Res 2006;326:553-72.
- Werry TD, Loiacono R, Sexton PM, et al. RNA editing of the serotonin 5HT2C receptor and its effects on cell signalling, pharmacology and brain function. Pharmacol Ther 2008;119:7-23.
- Villalón CM, Centurión D. Cardiovascular responses produced by 5-hydroxytriptamine:a pharmacological update on the receptors/mechanisms involved and therapeutic implications. Naunyn Schmiedebergs Arch Pharmacol 2007;376:45-63.
- Ramage AG, Villalón CM. 5-hydroxytryptamine and cardiovascular regulation. Trends Pharmacol Sci 2008;29:472-81.
5-HT4 receptor
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gastro-oesophageal reflux, constipation and constipation-predominant irritable bowel syndrome (IBS-c), before they were withdrawn due to cardiovascular side-effects.Excerpt from IUPHAR/BPS Guide to Pharmacology Related Receptors
Filters Sort resultsReset Apply
Human Human Human Human Human Human Human Human Human Human Human Human Mouse Mouse Mouse Mouse Mouse Mouse Mouse Mouse Mouse Mouse Mouse