Serotonin 5-hydroxytryptamine 2A, 2B, and 2C receptor (5-HT2A, 5-HT2B, and 5-HT2C receptor)

The Serotonin 5-hydroxytryptamine 2A, 2B, and 2C receptors are closely related members of the serotonin receptor family, classified as G protein-coupled receptors (GPCRs). They are widely distributed in the central nervous system and peripheral tissues, mediating the effects of serotonin on mood, cognition, vascular tone, appetite, and other physiological processes. Structurally, these receptors are characterized by seven transmembrane domains and specific ligand-binding pockets. The 5-HT2A receptor is particularly notable as the principal target of hallucinogenic drugs and atypical antipsychotics, while 5-HT2C is a drug target in appetite regulation and obesity, and 5-HT2B plays a key role in cardiac function. Drugs that interact with these receptors include both agonists (producing receptor activation) and antagonists/inverse agonists (blocking receptor signaling), with both therapeutic and adverse effects rooted in their mechanism of action. The balance of activation among 5-HT2A, 5-HT2B, and 5-HT2C is critical for neuropsychiatric functions and cardiovascular health.

Other names

5-HT2A receptor5-HT2B receptor5-HT2C receptorSerotonin receptor 2A/2B/2CHTR2A, HTR2B, HTR2C (gene symbols)5-hydroxytryptamine receptor 2A/2B/2C

Agonists activate Gq/11-coupled signaling, increasing inositol phosphate turnover and calcium signaling. Antagonists/inverse agonists block signaling, attenuating neurotransmitter effects (e.g., antipsychotics on 5-HT2A). Some drugs have functional selectivity, selectively recruiting β-arrestin pathways or influencing receptor trafficking.