Neuropeptide Receptors - Drug Development

Abstract

Neuropeptide receptors represent a large segment of 7 transmembrane domain (7TM) G-protein-coupled receptors expressed in the central nervous system and in the periphery. These receptors are important drug targets for therapies of mental illness, metabolic diseases, and pain. The endogenous ligands are peptides of 5-60 amino acids and thus carry multiple pharmacophores that participate in the agonist action. The development of low molecular weight nonpeptide antagonists has been rapid, while development of low molecular weight agonists has been much more difficult. Despite these difficulties several dozen neuropeptide receptor ligands are in clinical development, as discussed here. © 2009 El..