5-HT4 receptor
Protein-coding gene in the species Homo sapiens From Wikipedia, the free encyclopedia
5-Hydroxytryptamine receptor 4 is a protein that in humans is encoded by the HTR4 gene.[5][6]
Function
This gene is a member of the family of human serotonin receptors, which are G protein-coupled receptors that stimulate cAMP production in response to serotonin (5-hydroxytryptamine). The gene product is a glycosylated transmembrane protein that functions in both the peripheral and central nervous system to modulate the release of various neurotransmitters. Multiple transcript variants encoding proteins with distinct C-terminal sequences have been described, but the full-length nature of some transcript variants has not been determined.[7]
Location
The receptor is located in the alimentary tract, urinary bladder, heart and adrenal gland as well as the central nervous system (CNS).[8] 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, pontine nuclei, and some areas of the thalamus. It has not been found in the cerebellum.[9]
Isoforms
Internalization is isoform-specific.[10]
Ligands
Summarize
Perspective
Several drugs that act as 5-HT4 selective agonists have recently been introduced into use in both scientific research and clinical medicine. Some drugs that 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.[11] Amongst these agonists prucalopride has >150-fold higher affinity for 5-HT4 receptors than for other receptors.
SB-207,145 radiolabeled with carbon-11 is used as a radioligand for 5-HT4 in positron emission tomography pig[12] and human[13] studies.
Agonists
- Tropisetron[14] – partial agonist
- BIMU-8
- Cisapride
- CJ-033,466 – partial agonist
- Felcisetrag
- ML-10302[15]
- Mosapride
- Prucalopride
- Renzapride
- RS-67506
- RS-67333 – partial agonist
- SL65.0155 – partial agonist
- Tegaserod
- Zacopride
- Metoclopramide
- Sulpiride
- Naronapride
- Usmarapride
Antagonists
- L-lysine
- Piboserod
- GR-113,808 (1-methyl-1H-indole-3-carboxylic acid, [1-[2-[(methylsulfonyl)amino]ethyl]-4-piperidinyl]methyl ester)[16]
- 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[17]
- Chamomile (ethanol extract)[18]
See also
References
Further reading
External links
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