Serotonin 5-hydroxytryptamine 2A receptor and Serotonin 5-hydroxytryptamine 2C receptor (5-HT2A receptor and 5-HT2C receptor)

Serotonin 5-hydroxytryptamine 2A receptor and 5-hydroxytryptamine 2C receptor are closely related members of the class A G protein-coupled receptor family. They mediate the effects of serotonin in the central nervous system, especially in regions governing cognition, mood, and perception. 5-HT2A and 5-HT2C receptors share primary sequence similarities and activate intracellular signaling mostly via Gq proteins, which, in turn, trigger phospholipase C pathways and result in downstream neurotransmission, gene expression changes, and cellular adaptation. The 5-HT2A receptor is heavily implicated in the pharmacology of hallucinogens and antipsychotics, while 5-HT2C is targeted for obesity and addiction therapies. Both receptors are significant in disorders of mood, cognition, and neuropsychiatric disease, and are frequent molecules of interest in drug discovery

Other names

5-HT2A receptor5-HT2C receptorHTR2AHTR2CSerotonin receptor 2ASerotonin receptor 2C

Agonism (activation): induces receptor coupling to Gq protein, triggering intracellular signaling (mainly PLC pathway) Antagonism: blocks receptor activity, prevents serotonin-mediated signaling Inverse agonism: stabilizes the inactive receptor state, reduces baseline activity