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5-hydroxytryptamine receptor 4 is a protein that in humans is encoded by the HTR4 gene.[1][2]
Location The receptor is located in the alimentary tract, urinary bladder, heart and adrenal gland as well as the central nervous system (CNS).[3] In the CNS the receptor appears in the putamen, caudate nucleus, nucleus accumbens, globus pallidus and substantia nigra and to a lesser extent in the neocortex, raphe and pontine nuclei and some areas of the thalamus. It has not been found in the cerebellum.[4] Isoforms Internalization is isoform-specific.[5] Ligands Several drugs which act as 5-HT4 selective agonists have recently been introduced into use in both scientific research and clinical medicine. Some drugs which act as 5-HT4 agonists are also active as 5-HT3 antagonists, such as mosapride, metoclopramide, renzapride and zacopride, and so these compounds cannot be considered highly selective. Research in this area is ongoing.[6] SB-207,145 radiolabeled with carbon-11 is used as a radioligand for 5-HT4 in positron emission tomography pig[7] and human[8] studies. Agonists Antagonists - Piboserod
- GR-113,808 (1-methyl-1H-indole-3-carboxylic acid, [1-[2-[(methylsulfonyl)amino]ethyl]-4-piperidinyl]methyl ester)[10]
- GR-125,487
- RS-39604 (1-[4-Amino-5-chloro-2-(3,5-dimethoxyphenyl)methyloxy]-3-[1-[2-methylsulphonylamino]piperidin-4-yl]propan-1-one)
- SB-203,186
- SB-204,070
- ([Methoxy-11C]1-butylpiperidin-4-yl)methyl 4-amino-3-methoxybenzoate[11]
- Chamomile (ethanol extract)[12]
See also References External links Further reading - Licht CL, 2009, Changes in the 5-HT4 receptor in animal models of depression and antidepressant treatment, PhD thesis, University of Copenhagen.
pt:Receptor 5-HT4 sr:5-HT4 receptor
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