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

The **5-hydroxytryptamine receptor 2A** (5-HT2A) and **5-hydroxytryptamine receptor 2C** (5-HT2C) are closely related members of the serotonin receptor family and function as G protein-coupled receptors (GPCRs) primarily coupling to Gq/11 proteins. Both are widely distributed in the central nervous system and peripheral tissues, with 5-HT2A being highly expressed in the cerebral cortex and involved in mood regulation, cognition, and perception, including the effects of hallucinogens, while 5-HT2C is found in the CNS and periphery and is important for mood, appetite, and metabolic regulation. Dysregulation of these receptors is implicated in numerous neuropsychiatric disorders, and both serve as important drug targets for antipsychotics, antidepressants, and anti-obesity agents. Hallucinogens (e.g., LSD, psilocin) produce their psychoactive effects primarily via 5-HT2A receptor activation, whereas antagonists at these sites are used for the treatment of schizophrenia and mood disorders. Both receptors display complex signaling, functional selectivity, and regulatory dynamics, which influence their physiological and therapeutic roles[1][2][3][4][5].

Other names

5-HT2A receptor5-HT2C receptorSerotonin receptor 2ASerotonin receptor 2CSerotonin 2A receptorSerotonin 2C receptor

Agonist at 5-HT2A/2C: induces hallucinogenic, cognition-enhancing, and anxiolytic effects by activating Gq protein-coupled pathways and intracellular signaling (e.g., IP3, diacylglycerol)[1][2][5]. Antagonist at 5-HT2A/2C: antipsychotic and antidepressant effects by blocking serotonin signaling in central nervous system pathways [1][5]. Functional selectivity/bias agonism: different ligands selectively activate distinct downstream pathways via the same receptor subtype, contributing to variability in clinical effects [1][2][5].