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

Serotonin receptor 1B and serotonin receptor 1D are closely related members of the G protein-coupled receptor (GPCR) superfamily, activated by the neurotransmitter serotonin (5-hydroxytryptamine, 5-HT). Both are primarily located in the central nervous system and on cerebral blood vessels. They mediate inhibitory neurotransmission by reducing intracellular cAMP levels, with presynaptic autoreceptor activity that controls serotonin release. These receptors are clinically validated targets for antimigraine drugs ("triptans"), leveraging their capacity to induce vasoconstriction and inhibit trigeminal pain pathways. Moreover, alterations in their function or expression have been implicated in depression, anxiety, and other neuropsychiatric disorders. Selective agonists and antagonists for 5-HT1B and 5-HT1D contribute to therapeutic modulation in migraine, depression, and potentially other CNS disorders

Other names

5-hydroxytryptamine receptor 1B5-HT1BHTR1B5-hydroxytryptamine receptor 1D5-HT1DHTR1DSerotonin receptor 1BSerotonin receptor 1D

Agonists: Induce vasoconstriction of cranial blood vessels; inhibit trigeminal nerve transmission; inhibit release of serotonin and other neurotransmitters through Gi/Go-coupled inhibition of adenylyl cyclase Antagonists/Inverse agonists: Increase serotonin in the synaptic cleft; potential antidepressant mechanism