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

5-hydroxytryptamine receptor 1B and 1D are closely related molecular targets within the serotonin receptor family, classified structurally as G protein-coupled receptors (GPCRs) with seven transmembrane domains[1][3][5]. Both function primarily as presynaptic inhibitory receptors, modulating serotonin and several other neurotransmitter releases in the central nervous system and peripheral tissues[7][8]. Physiologically, these receptors are essential for signal transduction in neural circuits governing mood, aggression, and other cognitive functions, as well as for mediating vasoconstriction in cerebral and meningeal blood vessels[5][7]. Their therapeutic relevance is underscored by their role as primary targets for antimigraine drugs (triptans and ergot alkaloids) and growing interest in disorders of mood and addiction[2][4][5][7]. Molecularly, they may exist as homodimers or heterodimers and display high ligand and sequence homology[6]. Notably, their expression and pharmacological responses can vary by brain region and across species, impacting both their clinical utility and drug safety profile[1][5].

Other names

5-HT₁B receptor5-HT₁D receptorSerotonin receptor 1BSerotonin receptor 1DHTR1BHTR1D

Agonists activate Gi/o proteins, inhibiting adenylate cyclase and decreasing cAMP formation, leading to reduced release of serotonin and other neurotransmitters[1][2][3]. Antagonists block receptor activity, potentially increasing serotonin levels[3][5]. Agonist-induced vasoconstriction (therapeutically exploited to abort migraine attacks)[5][7]. Autoreceptor activation inhibits serotonin release; heteroreceptor activation inhibits release of acetylcholine, glutamate, GABA, and noradrenaline[5].