Abstract

The prevalence of obesity continues to increase throughout the world and the burden of obesity and related co-morbidities is large. However, existing drug therapies for obesity are limited, and agents with high efficacy, safety and tolerability are expected to better meet patient needs and lead to more substantial commercial success. Neuropeptide Y (NPY) is thought to have a major role in the physiological control of energy homeostasis. Multiple receptor subtypes mediate the effects of NPY on energy homeostasis and many pharmacological studies indicate the involvement of Y1 and Y5 receptor subtypes in NPY-induced feeding and obesity. In addition, recent observations with gut-derived peptides suggest a role for Y2 and Y4 receptor subtypes as catabolic receptors. This article highlights and reviews recent observations and patents regarding NPY receptor ligands for drug discovery as antiobesity agents.

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