Target intelligence / Profile preview

Serotonin 5-hydroxytryptamine 4 Receptor (5-HT4)

Target
5-HT4
Molecular classification
GPCR, Serotonin receptor
01

Overview

The serotonin 5-HT4 receptor is a G protein-coupled receptor (GPCR) that binds the neurotransmitter serotonin (5-hydroxytryptamine, or 5-HT). It is encoded by the HTR4 gene. The receptor is a glycosylated transmembrane protein and exists in multiple isoforms. It modulates the release of various neurotransmitters and plays a role in cognition, mood regulation, appetite, and gastrointestinal motility. Agonists targeting this receptor are being explored for cognitive impairment, depression, and gastrointestinal motility disorders.

Other names
5-Hydroxytryptamine receptor 4HTR4
02

Mechanism of action

Agonists stimulate adenylyl cyclase activity and increase intracellular cAMP, leading to enhanced neuronal excitability and increased acetylcholine release.

03

Biological functions

Signal transductionNeurotransmitter modulationNeuroplasticityNeurogenesisRegulation of gastrointestinal motility
04

Disease associations

Cognitive impairmentDepressionGastrointestinal motility disordersChronic constipationIrritable bowel syndrome (IBS)

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