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5-Hydroxytryptamine 2B Receptor (5-HT2B Receptor)

Target: 5-HT2B Receptor
Molecular classification: G protein-coupled receptor (GPCR), Receptor, Class A/1 rhodopsin-like GPCR

Overview

The 5-hydroxytryptamine 2B receptor (5-HT2B receptor) is a G protein-coupled receptor that belongs to the serotonin receptor family. It is involved in various physiological processes, including cardiovascular function, neurotransmitter regulation, and cell cycle progression. Dysregulation of this receptor is implicated in diseases such as cardiac valvulopathy, pulmonary hypertension, psychiatric disorders, and cancer. Several drugs acting on this receptor have been withdrawn due to safety concerns regarding valvular heart disease.

Other names: Serotonin 5-HT2B ReceptorHTR2BSerotonin 5‑HT₂F Receptor (historical synonym)

Mechanism of action

Activation of Gq proteins leading to increased intracellular calcium and downstream signaling cascades (e.g., MAPK/ERK). Modulation of serotonin transporter function. β-arrestin recruitment.

Biological functions

Signal transductionRegulation of cardiac structure and functionModulation of neurotransmitter uptakeCell cycle regulationSmooth muscle contractionAutoreceptor function

Disease associations

Cardiac ValvulopathyPulmonary HypertensionBipolar I DisorderObsessive-Compulsive DisorderDepressionCancer

Safety considerations

Drug-induced valvular heart disease (with potent agonists)Potential for pathological proliferation of valve fibroblastsRisk associated with overactive receptor in pulmonary hypertension

Interacting drugs

Serotonin

2 more in the full profile.

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