Serotonin 5-hydroxytryptamine receptor 1B and Serotonin 5-hydroxytryptamine receptor 1D (5-HT1B and 5-HT1D receptor)

Serotonin 5-HT1B and 5-HT1D receptors are closely related G protein-coupled receptors (GPCRs) within the serotonin receptor family, featuring seven transmembrane domains and coupling predominantly to Gi or Go proteins. They are primarily expressed in presynaptic neurons in the central nervous system, where they function as inhibitory autoreceptors to modulate the synaptic release of serotonin and other neurotransmitters. Both receptors have key roles in the regulation of vascular tone, especially affecting cerebral blood vessels and mediating vasoconstriction, which is the therapeutic basis for triptan-class drugs' efficacy in migraine therapy. Additionally, 5-HT1B/1D receptors are implicated in numerous neuropsychiatric and vascular conditions, with drugs acting as agonists or antagonists exerting antidepressant, anxiolytic, and vascular-modulating effects. Selectivity and affinity for these receptor subtypes determine clinical effect profiles and safety, with notable concerns for cardiovascular adverse events associated with their pharmacological activation.

Other names

5-HT1B receptor5-HT1D receptorSerotonin receptor 1BSerotonin receptor 1DHTR1B (gene, human)HTR1D (gene, human)

Agonists: activate 5-HT1B/1D receptors, causing presynaptic inhibition and reduced neuropeptide release in cranial blood vessels, leading to vasoconstriction and migraine relief. Antagonists/inverse agonists: block or suppress receptor activity, may increase serotonin release and have potential antidepressant activity