Serotonin receptor (5-HT1A, 5-HT1B, 5-HT1E, 5-HT1F, 5-HT2C, 5-HT5A, 5-HT7) (5-HTR (1A/1B/1E/1F/2C/5A/7))

The serotonin receptor group comprising subtypes 5-HT1A, 5-HT1B, 5-HT1E, 5-HT1F, 5-HT2C, 5-HT5A, and 5-HT7 represents a diverse set of G protein-coupled receptors (GPCRs) primarily located within the central and peripheral nervous systems. These receptors mediate the effects of the neurotransmitter serotonin (5-hydroxytryptamine) and are involved in a wide array of physiological processes, including mood regulation, sleep-wake cycles, appetite, and vascular tone. For instance, 5-HT1A and 5-HT7 are heavily implicated in depression and anxiety, while 5-HT1B and 5-HT1F are critical targets for migraine therapy due to their roles in cranial vasoconstriction and trigeminal inhibition. The 5-HT2C receptor is a well-known regulator of satiety and energy balance, making it a target for anti-obesity medications. Pharmacological intervention across these subtypes varies significantly; drugs may act as selective agonists, such as lasmiditan for 5-HT1F, or as multimodal agents like vortioxetine, which modulates several of these receptors simultaneously to treat major depressive disorder. Understanding the specific distribution and signaling pathways of these individual subtypes is essential for developing targeted therapies with minimized side effects, such as avoiding the cardiovascular risks associated with non-selective 5-HT1B activation.

Other names

5-Hydroxytryptamine receptors5-HT receptorsSerotonin receptor subtypes5HT1A5HT1B5HT1E5HT1F5HT2C5HT5A5HT7

Drugs targeting these receptors function through various mechanisms including orthosteric agonism, partial agonism, and antagonism to modulate downstream G-protein signaling (Gi/o, Gq/11, or Gs) and arrestin recruitment [IUPHAR/BPS Guide to Pharmacology].