Serotonin 5-hydroxytryptamine 2C receptor (5-HT2C receptor)

The serotonin 5-hydroxytryptamine 2C receptor (5-HT2C receptor) is a G protein-coupled receptor (GPCR) encoded by the HTR2C gene, primarily expressed in the central nervous system, notably in the choroid plexus, hippocampus, brainstem nuclei, and other brain regions[3][7]. It mediates excitatory neurotransmission via coupling to Gq/11 proteins, activating phospholipase C and increasing intracellular calcium[4][5]. The receptor plays a crucial role in regulating mood, anxiety, appetite, neuroendocrine secretions, and reward pathways, and is implicated in the pathophysiology of neuropsychiatric and metabolic disorders[3][6]. Therapeutic drugs that act as agonists or antagonists/inverse agonists at this receptor are used or investigated for obesity, depression, and psychosis. The 5-HT2C receptor undergoes RNA editing and alternative splicing, generating functionally distinct isoforms, and contains genetic variants such as the Cys23Ser polymorphism, which can affect drug response and disease risk[4][5]. Notable interacting drugs include lorcaserin (agonist, for obesity), various antipsychotics (antagonists), and psychedelic compounds[1][2][3]. Therapeutic modulation carries risks of psychiatric and metabolic side effects.

Other names

HTR2C5-HT2CRSerotonin receptor 2CHydroxytryptamine receptor 2C

Agonism at 5-HT2C receptor (e.g., lorcaserin, psilocin) - Inverse agonism or antagonism at 5-HT2C receptor (e.g., ritanserin, mirtazapine, olanzapine, clozapine)