The making of the 5-HT2C receptor

Abstract

This chapter is a personal account of how the 5-HT2C receptor was discovered and characterized more than 25 years ago. 5-HT2C receptors, initially called 5-HT1C, were found while studying the distribution in the brain of binding sites for the compound mesulergine, a ligand with serotonergic and dopaminergic properties. The strong labeling to choroid plexus revealed a site with pharmacological properties different from the known 5-HT receptors at that time. In the following 10 years, 5-HT1C (later 5-HT2C) was extensively characterized pharmacologically, anatomically, and functionally, leading finally to the cloning of its gene. Since then, intense research has been dedicated to the search a therapeutic use for modulators of these receptors.