5-Hydroxytryptamine receptor 4 is a protein that in humans is encoded by the HTR4 gene.[5][6]
HTR4 | |||||||||||||||||||||||||||||||||||||||||||||||||||
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Aliases | HTR4, 5-HT4, 5-HT4R, 5-HT4 receptor, 5-hydroxytryptamine receptor 4 | ||||||||||||||||||||||||||||||||||||||||||||||||||
External IDs | OMIM: 602164 MGI: 109246 HomoloGene: 20243 GeneCards: HTR4 | ||||||||||||||||||||||||||||||||||||||||||||||||||
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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]
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]
Internalization is isoform-specific.[10]
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.
This article incorporates text from the United States National Library of Medicine, which is in the public domain.