5-hydroxytryptamine receptor 2C (HTR2C) (HTR2C)

The 5-hydroxytryptamine receptor 2C (5-HT2C) is a G protein-coupled receptor (GPCR) primarily expressed in the central nervous system, particularly in the choroid plexus, hypothalamus, and limbic system (UniProt P28335). It plays a critical role in regulating various physiological processes, including appetite, mood, anxiety, and endocrine function (PubMed PMID: 21629138). Dysregulation of 5-HT2C signaling is implicated in several neuropsychiatric disorders such as depression, schizophrenia, and obesity (StatPearls: Serotonin Receptors). Pharmacologically, 5-HT2C is a significant therapeutic target; agonists like lorcaserin have been used for weight management by promoting satiety, while many atypical antipsychotics and antidepressants act as antagonists or inverse agonists at this site (NIH: PubChem). The receptor is also notable for its extensive post-transcriptional RNA editing, which can alter its G protein coupling efficiency and constitutive activity (PubMed PMID: 15554885). Furthermore, its modulation of dopaminergic and noradrenergic pathways makes it a key focus for developing treatments for addiction and impulse control disorders.

Other names

5-HT2C receptorSerotonin receptor 2C5-HT-2CHTR2C5-hydroxytryptamine receptor 2C5-HT2CR

The 5-HT2C receptor is a Gq-coupled GPCR that activates phospholipase C, leading to increased intracellular calcium. In the hypothalamus, 5-HT2C agonism stimulates POMC neurons to release alpha-MSH, which activates MC4 receptors to induce satiety (PubMed PMID: 21629138). Antagonism of 5-HT2C receptors in the prefrontal cortex and limbic system increases the synaptic availability of dopamine and norepinephrine, contributing to the efficacy of certain antidepressants and antipsychotics (StatPearls).