Target intelligence / Profile preview

Serotonin 5-HT2B Receptor (5-HT2B)

Target
5-HT2B
Molecular classification
G protein-coupled receptor (GPCR), Receptor, GPCR Class A
01

Overview

The serotonin 5-HT2B receptor is a G protein-coupled receptor activated by serotonin. It plays roles in cardiac valve maintenance, serotonergic tone modulation, vascular contraction, and behavioral/mood regulation. Overactivation can lead to valvulopathy, while antagonism may have antidepressant properties. It is expressed in the CNS, cardiac valve leaflets and blood vessels. Activation stimulates phospholipase C, increasing intracellular calcium.

Other names
5-hydroxytryptamine receptor 2BHTR2B
02

Mechanism of action

Gq protein activation leading to PLC activation, increased intracellular calcium, and downstream signaling pathways such as MAPK/ERK. Can also modulate serotonergic and dopaminergic neurotransmission.

03

Biological functions

Signal transductionCardiac valve maintenanceSerotonergic tone modulationVascular contractionBehavioral/mood regulationRegulation of serotonin releaseCell proliferation
04

Disease associations

Cardiovascular diseaseMood disordersValvulopathyDepression
05

Safety considerations

Valvular heart disease due to overstimulationCardiotoxicity
06

Interacting drugs

Serotonin

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