Serotonin 5-HT2 receptor (5-HT2 receptor)

The serotonin 5‑HT₂ receptors are a subfamily of G protein-coupled receptors that mediate many central nervous system functions by responding primarily to the neurotransmitter serotonin (5-hydroxytryptamine). The best-characterized member is the serotonin 5‑HT₂A receptor. These receptors are coupled mainly via Gq/G11 proteins that activate phospholipase C signaling pathways leading to increased intracellular calcium levels. They play key roles in modulating mood, cognition, perception, sleep-wake cycles, platelet aggregation, vascular tone regulation, and are implicated in psychiatric conditions such as schizophrenia and depression as well as substance use disorders. Many clinically important drugs—including atypical antipsychotics—act by blocking these receptors. Psychedelic compounds like LSD exert their characteristic effects primarily through activation of cortical serotonin 5‑HT₂A receptors.

Other names

5-hydroxytryptamine 2 receptor5-HT2A receptor (for the most studied subtype)Serotonin receptor 2HTR2 (gene family abbreviation)

Antagonists block serotonin binding to the receptor to reduce excitatory neurotransmission; used in antipsychotic therapy and migraine prevention. Agonists activate the receptor to induce changes in perception and mood; this is the primary mechanism for psychedelic effects. Some drugs act as inverse agonists or partial agonists depending on their structure.