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The 5-HT2C receptor is a G protein-coupled receptor (GPCR) that primarily couples to the Gq/G11 protein and mediates excitatory neurotransmission. It plays significant roles in regulating mood, anxiety, feeding behavior, and reproductive behavior. It also modulates dopamine release across several brain regions. Genetic variations are associated with susceptibility to psychiatric disorders, substance use disorders, and obesity. Drugs targeting the 5-HT2C receptor are used or investigated for treating obesity, drug abuse, and schizophrenia. Antagonists can stimulate dopaminergic pathways, potentially useful for counteracting SSRI-induced side effects or treating Parkinson’s disease. The receptor interacts with proteins such as MPDZ, which may influence its signaling properties.
Agonism, antagonism, inverse agonism, allosteric modulation, depending on the drug and region of the brain.
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