5-hydroxytryptamine 1 receptor (5-HT1 receptor)

The 5-hydroxytryptamine 1 receptor (5-HT1 receptor) refers to a subfamily of G protein-coupled receptors (GPCRs) that bind serotonin, a key neurotransmitter in the CNS and periphery. This subfamily includes subtypes 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, and 5-HT1F receptors, all characterized by seven transmembrane domains that couple to Gi/Go proteins, leading to inhibitory signaling via reduced cyclic AMP and regulation of ion channels. Found in both the CNS and peripheral tissues, these receptors play central roles in modulating neurotransmitter release, mood, anxiety, pain, and cognition. They are validated therapeutic targets for drugs treating migraine, anxiety, depression, and other neuropsychiatric conditions. Examples of interacting drugs include triptans (antimigraine) and buspirone (anxiolytic). Safety concerns involve cardiovascular risks (especially with triptans), CNS effects, and the potential for serotonin syndrome when co-administered with other serotonergic agents.

Other names

Serotonin 1 receptor5-HT1A receptor5-HT1B receptor5-HT1D receptor5-HT1E receptor5-HT1F receptorHTR1AHTR1BHTR1DHTR1EHTR1F

Agonists: inhibit adenylyl cyclase, hyperpolarize neurons, reduce neurotransmitter release, promote vasoconstriction (5-HT1B/1D). Antagonists: block inhibitory effects, potentially modulate cognition, mood, and other central functions. Partial agonists: modulate serotonergic tone without full receptor activation.