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

The 5-hydroxytryptamine receptor 2A (5-HT2A) is a G protein-coupled receptor (GPCR) that serves as a major excitatory serotonin receptor subtype in the mammalian brain (UniProt P28223). It is highly expressed in the cerebral cortex and is involved in the regulation of mood, perception, and cognitive functions (PubMed: 29108214). In clinical practice, the 5-HT2A receptor is a critical target for atypical antipsychotics like olanzapine, which bind as antagonists or inverse agonists to mitigate the positive and negative symptoms of schizophrenia (StatPearls: Antipsychotic Medications). Beyond the central nervous system, the receptor plays roles in platelet aggregation and smooth muscle contraction (NCBI Gene: 3356). Its involvement in the mechanism of action of psychedelic drugs further highlights its role in modulating consciousness and sensory processing (PubMed: 32315354). Dysregulation of 5-HT2A signaling is implicated in various neuropsychiatric conditions, including major depressive disorder and anxiety (PubMed: 29108214). Therapeutic modulation of this receptor remains a cornerstone of modern psychopharmacology, balancing efficacy in symptom control with the management of side effects.

Other names

HTR2ASerotonin receptor 2A5-HT2A5-hydroxytryptamine receptor 2A

Atypical antipsychotics like olanzapine act as potent antagonists or inverse agonists at the 5-HT2A receptor, which is thought to contribute to their efficacy in treating psychosis while reducing the risk of extrapyramidal side effects compared to typical antipsychotics (PubChem: Olanzapine; PubMed: 32315354).