D. W. Smith and E. M. Parker* Pages 363 - 372 ( 10 )
Serotonin receptors have been fertile targets for drug development for decades. The attractiveness of serotonin receptors as drug targets is due to the wide range of physiological processes in which serotonin plays a role and to diversity of receptor subtypes that mediate the physiological effects of serotonin. The powerful combination of molecular cloning and pharmacology has thus far led to the identification of fifteen different serotonin receptor subtypes. Fourteen of these serotonin receptors are G protein coupled receptors and one is a ligand-gated ion channel. Because many of these serotonin receptor subtypes have been identified very recently, the current opportunities for development of d gs that act via these receptors are manifold. This chapter focuses on recent molecular insights into the structure and function of serotonin receptors, discusses the relevance of these insights to the design and discovery of receptor selective drugs and reviews recently discovered selective antagonists for serotonin receptors.