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

Serotonin receptor 1B and serotonin receptor 1D are closely related G protein-coupled receptors found primarily in the central nervous system and on blood vessels. Both function mainly as inhibitory presynaptic auto- and heteroreceptors, regulating the release of serotonin and other neurotransmitters. They are the principal therapeutic targets for antimigraine medications (triptans and ergot derivatives), which act as agonists to induce cranial vasoconstriction and block pain transmission. These receptors are also implicated in mood disorders, addiction, and cardiovascular diseases due to their diverse roles in neurotransmission and vascular tone. Drugs that interact with them require careful monitoring for cardiovascular safety due to vasoconstrictive effects. Molecularly, both display the typical seven-transmembrane structure of GPCRs, and structural studies have clarified important features for ligand selectivity and drug design.

Other names

5-HT1B receptor5-HT1D receptorSerotonin receptor 1BSerotonin receptor 1D5-hydroxytryptamine receptor 1B5-hydroxytryptamine receptor 1DHTR1BHTR1DMigraine receptor

Agonists: Activate the receptor to cause vasoconstriction in cranial blood vessels (e.g., triptans for migraine) Antagonists/inverse agonists: Block receptor, increasing synaptic serotonin concentration (explored as antidepressants) Inhibitory modulation of neurotransmitter release (presynaptic auto- and heteroreceptor activity)