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

Serotonin receptor 2A (5-HT2A) and serotonin receptor 2C (5-HT2C) are closely related G protein-coupled receptors (GPCRs) that bind the neurotransmitter serotonin (5-hydroxytryptamine, 5-HT) and couple primarily to the Gq/11 signaling cascade, resulting in excitatory neurotransmission and complex intracellular signaling. 5-HT2A is extensively distributed in the cortex, hippocampus, cardiovascular system, platelets, and other tissues, and plays key roles in cognition, perception, vascular tone, and the pharmacological effects of both psychedelic and antipsychotic drugs. 5-HT2C is primarily found in the central nervous system, especially the choroid plexus and areas regulating mood and appetite, with known involvement in psychiatric disorders, obesity, and unique patterns of genetic regulation such as X-linked inheritance and RNA editing[1][2][3][4][5][6][7]. These receptors are major therapeutic targets for antipsychotics, antidepressants, weight-loss agents, and hallucinogenic compounds, and are research foci in neuropsychiatric, metabolic, and cardiovascular diseases. Biochemically, they can form homo- and hetero-dimeric or higher-order complexes and influence diverse behavioral and physiological processes through widespread central and peripheral actions.

Other names

5-HT2A receptorHTR2ASerotonin receptor 2A5-HT2C receptorHTR2CSerotonin receptor 2CSerotonin 2A receptorSerotonin 2C receptor5-hydroxytryptamine receptor 2A5-hydroxytryptamine receptor 2C

Agonists at 5-HT2A/2C stimulate Gq/11-coupled signaling, increasing IP3/DAG and intracellular calcium signaling[1][7] Antagonists inhibit receptor-mediated neurotransmission and associated downstream effects[5][7] Psychedelics act primarily as 5-HT2A partial agonists to induce altered perception and cognition[1][5][7] Antipsychotics often act as 5-HT2A antagonists to reduce psychotic symptoms or as inverse agonists[4][5] 5-HT2C agonists (e.g., lorcaserin) decrease appetite and weight[3]