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The serotonin receptor subtype 1B (5-HT1B) is a G protein-coupled receptor that binds serotonin (5-hydroxytryptamine, 5-HT). It functions as a terminal autoreceptor on serotonergic neurons, regulating serotonin release by inhibiting further release when activated. Activation inhibits adenylyl cyclase activity, leading to decreased cAMP levels. It is primarily located in the basal ganglia, frontal cortex, and primary visual cortex. Medications acting on this target are primarily used for migraine treatment due to their ability to constrict cranial blood vessels. Homo- and hetero-dimerization with other serotonin receptors has been observed, but the physiological relevance is still under investigation.
Agonists at the 5-HT1B receptor cause vasoconstriction and inhibit the release of pro-inflammatory neuropeptides.
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