Serotonin Receptor 5HT2A (5-HT2A)

The serotonin receptor 5HT2A, also known as the 5-hydroxytryptamine receptor 2A or simply 5-HT2A, is a G protein-coupled receptor (GPCR) that binds the neurotransmitter serotonin (5-HT). It is one of the most widely expressed and studied serotonin receptors in both the central nervous system (CNS) and peripheral tissues. It is highly expressed in the CNS, especially in regions critical for learning, memory, cognition, and perception such as prefrontal cortex layer V pyramidal neurons. Also found peripherally: present on platelets, endothelial cells, smooth muscle cells—especially within cardiovascular tissues where it mediates vasoconstriction and inflammation responses. The 5HT2A receptor is a major target for several drug classes, including agonists (classic psychedelics) and antagonists/inverse agonists (many atypical antipsychotics, some antidepressants). Abnormal function or expression has been linked with psychiatric disorders including depression, schizophrenia, substance use disorders; it may also play roles in neurodegenerative diseases.

Other names

5-hydroxytryptamine receptor 2AHTR2A

Agonist (e.g., psychedelics) or antagonist/inverse agonist (e.g., antipsychotics) binding to the 5-HT2A receptor, modulating downstream signaling pathways via Gq/11 protein activation and subsequent effects on phospholipase C, diacylglycerol, inositol triphosphate, intracellular calcium release, and protein kinase C activation.