Serotonin 5-hydroxytryptamine 2A Receptor (5-HT2A)

The serotonin 2A receptor (5-HT2A) is a G protein-coupled receptor (GPCR) subtype of the serotonin receptor family. It is widely expressed in the central nervous system (CNS) and peripheral tissues. Upon activation, it primarily couples to Gαq proteins, leading to increased production of diacylglycerol (DAG) and inositol triphosphate (IP3), stimulating protein kinase C (PKC) activity and promoting intracellular calcium release. The receptor modulates mood regulation, perception, cognition, and vascular tone. Its dysregulation has been implicated in psychiatric disorders such as depression, schizophrenia, and drug addiction. It is a target for psychoactive substances like LSD and antipsychotic drugs.

Other names

Serotonin receptor 2A5-hydroxytryptamine receptor 2AHTR2A

Agonism, antagonism, or inverse agonism at the 5-HT2A receptor modulate downstream signaling pathways involving Gαq, phospholipase C (PLC), diacylglycerol (DAG), inositol triphosphate (IP3), protein kinase C (PKC), and intracellular calcium (Ca2+) release, influencing neurotransmitter release, gene expression, synaptic plasticity, and vasoconstriction.