5-hydroxytryptamine receptor 1B (5-HT1B) (5-HT1B)

The 5-hydroxytryptamine receptor 1B (5-HT1B) is a member of the G protein-coupled receptor (GPCR) superfamily that responds to the neurotransmitter serotonin. It is predominantly expressed in the central nervous system as a presynaptic autoreceptor or heteroreceptor, where it modulates the release of serotonin, glutamate, and GABA (UniProt P28222). In the vascular system, 5-HT1B receptors are found on smooth muscle cells of cranial blood vessels, where their activation induces vasoconstriction (IUPHAR/BPS Guide to Pharmacology). This vascular effect is the primary therapeutic mechanism for triptans, a class of drugs used to treat acute migraine attacks by reversing vasodilation and inhibiting trigeminal pain signaling (StatPearls). Additionally, 5-HT1B is linked to various behavioral and psychiatric conditions, including aggression, depression, and addiction, making it a target of interest for neuropsychiatric drug development (PubMed, PMID: 16273023). However, because of its presence in coronary arteries, drugs targeting this receptor must be used cautiously in patients with cardiovascular disease to avoid potential ischemic events.

Other names

HTR1BSerotonin receptor 1B5-HT-1B5-HT1DBS12h5-HT1B

Agonism of the 5-HT1B receptor leads to Gi/o protein-mediated inhibition of adenylate cyclase, resulting in decreased cAMP levels. In the context of migraine, this causes vasoconstriction of distended cranial extracerebral blood vessels and inhibits the release of pro-inflammatory neuropeptides from trigeminal nerve endings (StatPearls, PMID: 29939618).