Serotonin 5-HT2A, 5-HT2B, 5-HT2C, and 5-HT7 receptor (5-HT2A, 5-HT2B, 5-HT2C, 5-HT7 receptor)

The serotonin 5-HT2A, 5-HT2B, 5-HT2C, and 5-HT7 receptors are members of the G protein-coupled receptor family that mediate the cellular responses to the neurotransmitter serotonin. Structurally, they possess the canonical seven transmembrane α-helix architecture typical of class A GPCRs, with unique features in their ligand-binding domains that confer subtype selectivity. Functionally, these receptors are expressed in both central and peripheral tissues, where they regulate diverse biological processes including neurotransmitter release, mood, perception, neurodevelopment, cardiovascular function, and hormone regulation. They are major drug targets for psychiatric medications, hallucinogens, anti-obesity drugs, and other therapeutics. Each subtype has distinct patterns of expression and involvement in both normal physiology and disease states; notably, 5-HT2B activation carries a risk of cardiac toxicity, while 5-HT2A is central to the action of hallucinogens and some antipsychotics, and 5-HT2C and 5-HT7 play roles in mood regulation, cognition, and neurodevelopment. Grouping these as a single "target" is imprecise for most pharmacological or therapeutic contexts; each receptor should be addressed separately for specificity and accuracy.

Other names

5-HT2A receptor5-HT2B receptor5-HT2C receptor5-HT7 receptor5-HT2 familySerotonin receptor

Agonism or antagonism at the orthosteric ligand binding site; drugs can act as full agonists, partial agonists, antagonists, or inverse agonists. - Modulation of intracellular signaling cascades (primarily via Gq/11 proteins for 5-HT2A/2B/2C: phospholipase C activation, increased IP3/diacylglycerol, calcium release; 5-HT7 signals via Gs and increases cAMP) - Some drugs exhibit functional selectivity/biased agonism (different ligands preferentially activate certain signaling pathways—G protein vs. β-arrestin-mediated signaling)