The 5-Hydroxytryptamine type 2C receptor (5-HT2C, previously 5-HT1C) is a G protein-coupled receptor (GPCR) that is activated by serotonin, and is exclusively expressed in the central nervous system. To date, it is the only GPCR that undergoes adenosine-to-inosine RNA editing at five positions, generating multiple receptor isoforms that exhibit different G protein-coupling properties and trafficking. Alteration of editing may have a role in pathophysiological processes, such as depression. 5-HT2C receptors modulate a large variety of behavioral and physiological processes, such as regulation of mood, nociception, motor behavior, endocrine secretion, thermoregulation, modulation of appetite and secretion of cerebrospinal fluid. 5-HT2C receptors can interact with a variety of intracellular proteins, such as PDZ-containing proteins that have a critical influence on their trafficking, their desensitization and their coupling to the signaling machinery.