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Target intelligence / Profile preview
Serotonin 5-hydroxytryptamine Receptor 4 (5-HT4 Receptor)
- Target
- 5-HT4 Receptor
- Molecular classification
- G protein-coupled receptor, GPCR, Receptor
01
Overview
The 5-HT4 receptor is a serotonin receptor that stimulates cyclic adenosine monophosphate (cAMP) production in response to serotonin (5-hydroxytryptamine, 5-HT). Activation of this receptor modulates the release of various neurotransmitters and impacts several physiological processes. The primary signaling pathway involves coupling to Gs proteins, leading to activation of adenylate cyclase, increased cAMP levels, and subsequent activation of protein kinase A (PKA). It is expressed in the gastrointestinal tract, central nervous system, heart atria, and adrenal cortex. Agonists are used clinically for their prokinetic effects and it is implicated in mood regulation and potentially neurodegenerative diseases.
- Other names
- serotonin receptor 4serotonin type 4 receptorG-protein coupled serotonin receptor
02
Mechanism of action
Agonist of the 5-HT4 receptor, leading to increased cAMP production
03
Biological functions
Signal transductionModulation of gastrointestinal motilityRegulation of neurotransmitter releaseStimulates Ca²⁺ channelsInhibits K⁺ channelsActivates downstream pathways such as rap1-rac via cAMP/Epac signaling
04
Disease associations
Major depressive disorderNeurodegenerative diseasesAlzheimer’s diseaseParkinson’s diseaseChronic idiopathic constipationGERDGastroparesisIBS-CGI motility disorders
05
Interacting drugs
Prucalopride
3 more in the full profile.
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