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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.
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.
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