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

The 5-hydroxytryptamine 2C receptor (5-HT2C receptor) is a subtype of the 5-HT2 receptor that binds the endogenous neurotransmitter serotonin (5-hydroxytryptamine, 5-HT). It is a Gq/G11-coupled GPCR mediating excitatory neurotransmission. The receptor exists as a homodimer and its crystal structure is known. It is primarily located in the choroid plexus and various brain regions including hippocampus, substantia nigra, amygdala, and brainstem nuclei. The human gene, HTR2C, is on the X chromosome, meaning polymorphisms can affect sexes differently. It belongs to the Family A G protein-coupled receptors and the G-protein coupled receptor 1 family. It interacts with numerous ligands, including various agonists like lorcaserin and psychedelics. Structural studies have provided insights into its activation mechanism and polypharmacology. The receptor undergoes RNA editing at multiple sites. It has been explored as a therapeutic target, particularly in the context of substance use disorder (SUD).

Other names

HTR2C

The 5-HT2C receptor is a Gq/G11-coupled receptor that mediates excitatory neurotransmission. Upon binding of agonists like serotonin or other ligands, it undergoes conformational changes, including an outward tilt of helix VI and an inward shift of helix III, leading to receptor activation and downstream signaling.