Aminothiazole Derivatives as Neuropeptide Y5 Receptor Ligands: Finding the Balance between Affinity and Physicochemical Properties

摘要

Neuropetide Y is a peptide of 36 amino acids that is widely distributed in the central and peripheral nervous systems.It mediates a number of physiological effects through its various receptor subtypes.Studies in animals have shown that neuro-peptide Y is a powerful stimulus of food intake,and it has been demonstrated that the activation of neuropeptide Y5 (NPY5) receptors results in hyperphagia and decreased thermo-genesis.Therefore,compounds that antagonize neuropeptide Y at the Y5 receptor subtype might represent an approach to the treatment of eating disorders such as obesity and hyperphagia.Although it has been suggested that the antagonism of the NPY5 receptor does have a major effect on feeding in rats,there is evidence to support the NPY receptor system in humans as a valuable target for the treatment of metabolic disorders.