Serotonin 5-HT2A receptor and Serotonin 5-HT2C receptor (5-HT2A; 5-HT2C)

Serotonin 5-HT2A and 5-HT2C receptors are class A (rhodopsin-like) G protein-coupled receptors widely distributed in the central nervous system[1][2][5]. They are activated by the neurotransmitter serotonin and couple primarily to the phospholipase C signaling pathway, producing varied effects on neuronal signaling, mood, perception, memory, and cognition[3][5]. 5-HT2A receptors are key mediators of the effects of classical hallucinogens (e.g., LSD, psilocybin), while 5-HT2C receptors are implicated in mood regulation, appetite, and are targets for anti-obesity drugs[2][5]. They share structural similarity but differ in distribution, function, and therapeutic relevance. Drugs targeting these receptors exhibit therapeutic potential in neuropsychiatric disorders, though side effects and specific selectivity remain major challenges[1][2][5].

Other names

5-hydroxytryptamine receptor 2A (for 5-HT2A)5-hydroxytryptamine receptor 2C (for 5-HT2C)5-HT2A5-HT2CHTR2A (gene for 5-HT2A receptor)HTR2C (gene for 5-HT2C receptor)Classical D receptor (obsolete; for 5-HT2A)

Agonists activate signal transduction via Gq/11 protein, leading to phospholipase C activation and intracellular calcium release. Antagonists block receptor activation, dampening serotonin-mediated pathways. Some drugs show biased agonism, preferring certain downstream effects (e.g., β-arrestin signaling).