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

The Serotonin 2A receptor (5-HT2A) is a prominent G protein-coupled receptor primarily located in the central nervous system, particularly within the cerebral cortex, hippocampus, and basal ganglia [1]. It plays a critical role in modulating neuronal excitability, perception, and mood by signaling through the Gq/11 pathway to activate phospholipase C [1][4]. Dysregulation of 5-HT2A signaling is strongly linked to neuropsychiatric conditions, including schizophrenia and Parkinson's disease psychosis [3]. Unlike traditional antipsychotics that primarily target dopamine D2 receptors, drugs like pimavanserin selectively target the 5-HT2A receptor as inverse agonists and antagonists [2]. This selective modulation helps alleviate hallucinations and delusions without the motor side effects associated with dopamine blockade, making it a unique therapeutic option for neurodegenerative-related psychosis [2][4].

Other names

HTR2A5-HT2AR5-Hydroxytryptamine receptor 2ASerotonin receptor 2A

Inverse agonism and antagonism at the 5-HT2A receptor, which modulates downstream Gq-mediated signaling without affecting dopamine D2 receptors [2][3].