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Target intelligence / Profile preview
Serotonin 5-HT4 Receptor (5-HT4 receptor)
- Target
- 5-HT4 receptor
- Molecular classification
- G protein-coupled receptor, Receptor
01
Overview
The serotonin 5-HT4 receptor is a G protein-coupled receptor that mediates the effects of serotonin in both the peripheral and central nervous systems. It plays a key role in regulating gastrointestinal motility and modulating neurotransmitter release in the brain, influencing processes such as appetite, mood, and addiction. Agonists of this receptor are used clinically as prokinetic agents for gastrointestinal disorders like chronic idiopathic constipation and IBS-C.
- Other names
- 5-Hydroxytryptamine Receptor 4HTR4
02
Mechanism of action
Agonists of the 5-HT4 receptor stimulate cAMP production, leading to increased intestinal peristalsis. They also modulate neurotransmitter release in the central nervous system.
03
Biological functions
Signal transductionNeurotransmitter release modulationHormone release modulationRegulation of gastrointestinal motilityModulation of appetite and feeding behaviorsRegulation of reward circuits
04
Disease associations
Gastrointestinal disordersConstipationIrritable Bowel Syndrome with Constipation (IBS-C)AddictionMood disordersStress response
05
Safety considerations
Cardiovascular side effects (e.g., with Cisapride, leading to its withdrawal)Potential for psychiatric side effects given CNS involvement
06
Interacting drugs
Prucalopride
3 more in the full profile.
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