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Target intelligence / Profile preview
Serotonin Receptor 5-HT2B (5-HT2B)
- Target
- 5-HT2B
- Molecular classification
- G protein-coupled receptor (GPCR), Receptor
01
Overview
The serotonin receptor 5-HT2B is a G protein-coupled receptor (GPCR) that primarily signals through the Gq protein, leading to activation of downstream pathways such as phospholipase C and MAPK/ERK. It is expressed in the CNS and PNS, notably in cardiac valve leaflets where it is essential for normal development and maintenance. Overstimulation of this receptor is linked to drug-induced valvular heart disease. It is also implicated in mood disorders such as depression.
- Other names
- 5-hydroxytryptamine receptor 2BHTR2B
02
Mechanism of action
Agonists stimulate the receptor leading to Gq protein activation and downstream signaling via phospholipase C and MAPK/ERK pathways. Antagonists block receptor activation.
03
Biological functions
Signal transductionRegulation of vascular toneCardiac valve development and maintenanceModulation of neuronal excitabilityNeurotransmitter uptake inhibition
04
Disease associations
Valvular heart diseaseDepression
05
Safety considerations
Drug-induced valvular heart disease (with chronic agonist use)Potential for cardiac fibrosis with chronic overstimulation
06
Interacting drugs
SSRIs
6 more in the full profile.
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