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Target intelligence / Profile preview
5-Hydroxytryptamine Receptor 2B (5-HT2B)
- Target
- 5-HT2B
- Molecular classification
- G protein-coupled receptor, GPCR, Serotonin receptor
01
Overview
The 5-Hydroxytryptamine Receptor 2B (5-HT2B) is a G protein-coupled receptor that binds serotonin and other ligands. It plays key roles in cardiac regulation, vascular tone control, and neurotransmitter modulation. It is expressed in the CNS, heart valves, blood vessels, and other tissues. Its overstimulation is associated with valvulopathy and other diseases, making it a potential therapeutic target.
- Other names
- Serotonin Receptor 2BHTR2B
02
Mechanism of action
Ligand binding induces conformational changes, activating Gq/G11 proteins, which stimulate phospholipase C, increasing inositol phosphate hydrolysis and cytosolic calcium levels. Also engages PI3K/Akt and ERK/MAPK signaling cascades.
03
Biological functions
Cardiac regulationVascular tone controlNeurotransmitter modulationSerotonin homeostasisCell cycle progressionSignal transduction
04
Disease associations
Cardiovascular diseasePulmonary hypertensionLiver fibrosisMood disordersDepressionBipolar I disorderCancer
05
Safety considerations
Cardiac valvulopathy from chronic overstimulationPotential for off-target effects due to broad tissue distribution
06
Interacting drugs
Serotonin
3 more in the full profile.
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