Serotonin 5-HT2A Receptor (5-HT2A receptor)

The serotonin 5-HT2A receptor is a widely studied G protein-coupled receptor (GPCR) belonging to the 5-HT2 receptor family. It is highly expressed in the central nervous system, particularly in regions involved in cognition and learning, and also found in the cardiovascular system. It primarily signals via the Gαq pathway, generating IP3/DAG, AA, and 2-AG signals, and exhibits functional selectivity. The receptor plays crucial roles in neurotransmission, cognition, memory, mood, and cardiovascular function. It is implicated in several psychiatric disorders, including schizophrenia, depression, substance abuse disorders, and anxiety. Pharmacological targeting with both agonists and antagonists shows therapeutic potential for these conditions, though safety concerns like hallucinogenic effects of agonists and off-target effects of some antagonists exist.

Other names

D subtype of 5-HT receptors5-HT2

The 5-HT2A receptor primarily couples to the Gαq signal transduction pathway, leading to the activation of phospholipase C (PLC) and subsequent release of diacylglycerol (DAG) and inositol triphosphate (IP3), which stimulate protein kinase C (PKC) activity and Ca2+ release. The receptor also produces arachidonic acid (AA) and 2-arachidonylglycerol (2-AG) signals and displays functional selectivity, meaning different ligands can differentially activate these pathways. Agonists stimulate these pathways, often resulting in cognitive enhancement or hallucinogenic effects. Antagonists block receptor activation, leading to effects like antipsychotic or antidepressant actions.