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Serotonin Receptor Subtype 2B (5-HT2B)
- Target
- 5-HT2B
- Molecular classification
- G protein-coupled receptor, GPCR, Class A / Rhodopsin-like receptor
01
Overview
The 5-HT2B receptor is a G protein-coupled receptor (GPCR) primarily coupled to Gq/11, mediating diverse physiological functions. It plays a significant role in cardiac structure and function, vascular regulation, and neurotransmitter modulation in the CNS. A critical concern is its involvement in drug-induced valvular heart disease, making it an important off-target consideration in drug development for serotonergic agents. Overstimulation leads to pathological proliferation of cardiac valve fibroblasts leading to valvulopathy.
- Other names
- 5-HT₂BHTR2B
02
Mechanism of action
Gq/11 protein activation; stimulates phospholipase Cβ (PLCβ); generates diacylglycerol (DAG) & IP₃; increases intracellular Ca²⁺; activates protein kinase C (PKC)
03
Biological functions
Signal transductionCardiac development/homeostasisVascular tone regulationNeurotransmitter modulationSerotonin and dopamine uptake inhibitionRegulation of serotonin release via SERT modulation
04
Disease associations
Cardiovascular diseaseValvulopathyFibrosis disordersCancer
05
Safety considerations
Drug-induced valvular heart diseaseCardiotoxicityPotential for heart defects and ventricular hypertrophy with altered expression
06
Interacting drugs
Ergotamine
3 more in the full profile.
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