5-HT4 receptor

5-Hydroxytryptamine receptor 4 is a is_associated_with::protein that in humans is encoded by the HTR4 is_associated_with::gene.

Location
The receptor is located in the is_associated_with::alimentary tract, is_associated_with::urinary bladder, is_associated_with::heart and is_associated_with::adrenal gland as well as the is_associated_with::central nervous system (CNS). In the CNS the receptor appears in the is_associated_with::putamen, is_associated_with::caudate nucleus, is_associated_with::nucleus accumbens, is_associated_with::globus pallidus, and is_associated_with::substantia nigra, and to a lesser extent in the is_associated_with::neocortex, raphe, is_associated_with::pontine nuclei, and some areas of the is_associated_with::thalamus. It has not been found in the cerebellum.

Isoforms
Internalization is isoform-specific.

Ligands
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.

is_associated_with::SB-207,145 radiolabeled with is_associated_with::carbon-11 is used as a is_associated_with::radioligand for 5-HT4 in is_associated_with::positron emission tomography pig and human studies.

Agonists

 * is_associated_with::BIMU-8
 * is_associated_with::Cisapride
 * is_associated_with::CJ-033,466 - partial agonist
 * is_associated_with::ML-10302
 * is_associated_with::Mosapride
 * is_associated_with::Prucalopride
 * is_associated_with::Renzapride
 * RS-67506
 * is_associated_with::RS-67333 - partial agonist
 * is_associated_with::SL65.0155 - partial agonist
 * is_associated_with::Tegaserod
 * is_associated_with::Zacopride
 * is_associated_with::Metoclopramide
 * is_associated_with::Sulpiride

Antagonists

 * is_associated_with::Piboserod
 * is_associated_with::GR-113,808 (1-methyl-1H-indole-3-carboxylic acid, [1-[2-[(methylsulfonyl)amino]ethyl]-4-piperidinyl]methyl ester)
 * 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
 * is_associated_with::SB-204,070
 * ([Methoxy-11C]1-butylpiperidin-4-yl)methyl 4-amino-3-methoxybenzoate
 * Chamomile (ethanol extract)