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The serotonin receptor type 2C (5-hydroxytryptamine receptor 2C, abbreviated as 5‑HT₂C) is a member of the G protein-coupled receptor family that binds the endogenous neurotransmitter serotonin. It mediates excitatory neurotransmission via coupling to Gq/11 proteins. The human gene encoding this protein is HTR2C, located on the X chromosome. This receptor plays important roles in regulating mood, appetite control, endocrine secretion, motor function modulation, and cerebrospinal fluid volume regulation. It has been implicated in several neuropsychiatric disorders—including depression and anxiety—as well as obesity. Drugs targeting this site include both selective agonists and antagonists developed for research into CNS diseases and potential therapies for obesity. Polymorphisms within its gene can affect disease risk differently between sexes due to its X-linked inheritance pattern.
Drugs targeting this molecule act primarily by modulating serotonin signaling through the following mechanisms: - Agonism at the GPCR to stimulate downstream signaling via Gq/11 proteins, increasing IP3/DAG pathway activity and excitatory neurotransmission. - Antagonism or inverse agonism to block or reduce serotonin-mediated effects at this site.
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