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The serotonin 1B receptor (5-HT1B) is a G protein-coupled receptor (GPCR) primarily coupled to Gi/o proteins. It acts mainly as an inhibitory presynaptic receptor, inhibiting the release of serotonin and other neurotransmitters. It is involved in various physiological functions, including mood regulation, anxiety, aggression, and vasoconstriction, particularly in cerebral arteries. It is a target for triptan drugs used in acute migraine therapy.
Agonists suppress neurotransmitter release by decreasing cAMP formation. Antagonists/inverse agonists block the receptor or stabilize inactive conformations.
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