Serotonin 5-hydroxytryptamine receptor 1A (5-HT1A receptor) and Serotonin 5-hydroxytryptamine receptor 1D (5-HT1D receptor) (5-HT1A receptor, 5-HT1D receptor)

Serotonin 5-HT1A and 5-HT1D receptors are G protein-coupled receptors (GPCRs) of the serotonin receptor family, predominantly expressed in the central and peripheral nervous systems. These receptors are activated by the neurotransmitter serotonin (5-hydroxytryptamine) and play key roles in regulating mood, anxiety, aggression, and vascular tone. The 5-HT1A receptor is especially implicated in mood and anxiety regulation, making it a therapeutic target for antidepressants and anxiolytics. The 5-HT1D receptor is central to migraine pathophysiology and is targeted by triptan drugs that induce cranial vasoconstriction to treat migraines. Both receptors share a canonical seven-transmembrane domain architecture typical of class A GPCRs, with specific lipid and protein interactions modulating their function. Ligands and drugs may act as agonists, antagonists, or allosteric modulators to elicit therapeutic effects or side effects.

Other names

5-HT1A5-HT1DHTR1A (gene for 5-HT1A)HTR1D (gene for 5-HT1D)Serotonin receptor 1ASerotonin receptor 1D

Agonism (drugs activate the receptor to inhibit neurotransmitter release, induce vasoconstriction, or reduce pain transmission); Antagonism (less common; would block receptor activity); Partial agonism (e.g., buspirone for anxiolytic effect); Allosteric modulation (lipids and certain drugs may enhance or alter signaling efficacy)