5-hydroxytryptamine receptor 2A (5-HT2A) (5-HT2A)

The 5-hydroxytryptamine receptor 2A (5-HT2A) is a G protein-coupled receptor (GPCR) that serves as a primary mediator of serotonin's effects in the central nervous system and peripheral tissues (UniProt P28223). It is highly expressed in the cerebral cortex, where it influences cognitive processes, mood, and perception (PubMed PMID: 25839398). In the periphery, the receptor facilitates platelet aggregation and smooth muscle contraction (PubChem CID 54675798). Clinically, 5-HT2A is a critical target for atypical antipsychotics like clozapine and risperidone, which function as antagonists or inverse agonists to manage schizophrenia (StatPearls). Furthermore, it is the principal site of action for serotonergic psychedelics, which are being explored for treatment-resistant depression (PubMed PMID: 32760815). Dysregulation of this receptor is implicated in various neuropsychiatric disorders, including anxiety and obsessive-compulsive disorder.

Other names

HTR2ASerotonin 2A receptor5-HT2 receptor5-hydroxytryptamine receptor 2

Antagonism, inverse agonism, and agonism (partial and full) (StatPearls; PubMed PMID: 25839398)