Serotonin 5-hydroxytryptamine 2 receptor (5-HT2 receptor)

The serotonin 5-hydroxytryptamine 2 receptor (5-HT2 receptor) refers to a subfamily of G protein-coupled receptors (GPCRs) that bind the endogenous neurotransmitter serotonin (5-HT). This family includes three primary subtypes in humans: 5-HT2A, 5-HT2B, and 5-HT2C receptors[7][4][5]. They are expressed both centrally and peripherally, playing key roles in neuronal signaling, regulation of mood, cognition, vascular and smooth muscle tone, platelet aggregation, and various neuroendocrine functions[7][1][2]. The 5-HT2A receptor is most prominent in the central nervous system and is the principal target of classical hallucinogens (e.g., LSD, psilocybin, DMT) as well as atypical antipsychotics (e.g., risperidone, clozapine), with antagonists and inverse agonists having antipsychotic and antidepressant effects[1][2][10]. 5-HT2B activation is associated with cardiac adverse effects, while 5-HT2C is implicated in mood, appetite, and obesity[7]. These receptors primarily signal via the Gq/11 pathway, increasing IP3 and DAG, and their structure features the canonical seven-transmembrane helical bundle of class A GPCRs[1][3]. Agents targeting 5-HT2 receptors are of major therapeutic interest across neuropsychiatric, cardiovascular, and other disease domains, but therapeutic development is complicated by overlapping subtype selectivity and the risk of neuropsychiatric or cardiovascular side effects[2][7][6].

Other names

5-HT2 receptor5-HT2A receptor5-HT2B receptor5-HT2C receptor5HT25-HT2F (for 5-HT2B)5-HT1C (for 5-HT2C)D receptor (historical)

Agonism (stimulating the receptor), Antagonism (blocking the receptor), Inverse agonism (inducing opposite activity), Partial agonism (partial stimulation), Allosteric modulation