5-hydroxytryptamine receptor 1 family (5-HT1 receptor family) (5-HT1 receptor family)

The 5-hydroxytryptamine receptor 1 (5-HT1) family is a group of G protein-coupled receptors (GPCRs) that mediate the inhibitory effects of the neurotransmitter serotonin. This family includes five distinct subtypes: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, and 5-HT1F, all of which primarily signal through the Gi/o pathway to inhibit adenylate cyclase and reduce intracellular cAMP levels [1][2]. These receptors are widely expressed in the central nervous system, where they function as both presynaptic autoreceptors and postsynaptic receptors to modulate neuronal excitability and the release of various neurotransmitters [3]. Clinically, the 5-HT1 family is highly significant; for instance, 5-HT1A receptors are major targets for anxiolytic and antidepressant drugs, while 5-HT1B and 5-HT1D receptors are targeted by triptans to treat acute migraine attacks [4][5]. Dysregulation of these receptors is linked to a variety of conditions, including depression, anxiety, and movement disorders [6]. Recent drug development has also focused on 5-HT1F agonists as non-vasoconstrictive treatments for migraines [7]. The family's diverse roles in physiological processes like thermoregulation and blood pressure control further underscore its therapeutic importance [1].

Other names

5-HT1 receptorsSerotonin 1 receptors5-hydroxytryptamine 1 receptorsHTR1 family

Drugs targeting the 5-HT1 receptor family primarily act as agonists or partial agonists to mimic serotonin's inhibitory effects via Gi/o protein coupling, leading to decreased adenylate cyclase activity and reduced cAMP levels [1][3]. In migraine treatment, 5-HT1B/1D agonists induce cranial vasoconstriction and inhibit pro-inflammatory neuropeptide release from trigeminal nerves [5]. In psychiatry, 5-HT1A partial agonists modulate serotonergic tone to alleviate anxiety and depression [4].