NPY Y2 and Y4 receptors selective ligands: promising anti-obesity drugs?
Neuropeptide Y (NPY), a potent orexigen peptide widely produced and distributed in arcuate neurons in the hypothalamus, is a promising candidate for the control of appetitive ingestive behavior. In mammals, the signaling is mediated via at least five different cell surface receptors, denoted as Y(1), Y(2), Y(4), Y(5) and Y(6). Obesity is an important public health problem in the world, particularly in developed societies, and has taken on pandemic proportions. The therapeutics of obesity, including appetite suppressants, has increased 453% over the past decade, although issues concerning safety, efficacy, and little knowledge of the pharmacological activity result in the still modest effects of the anti-obesity drugs presently used. Ligands for Y receptors may be of benefit for the treatment of obesity, and recent findings have indicated a promising role of Y(2) and Y(4) in protecting against diet-induced obesity. This review highlights the supporting evidence therapeutic potential of Y(2) and Y(4) receptors antagonists as additional intervention to treat human obesity.
Kamiji
M M
MM
Department of Gastroenterology, Faculty of Medicine, University of Sao Paulo, Ribeirão Preto Campus, Ribeirão Preto, Brazil.
Inui
A
A
D000818:Animals; D019440:Anti-Obesity Agents / Q000494:pharmacology*; D005247:Feeding Behavior / Q000187:drug effects / Q000502:physiology; D006801:Humans; D008024:Ligands; D009765:Obesity / Q000188:drug therapy / Q000378:metabolism; D017476:Receptors, Neuropeptide Y / Q000037:antagonists & inhibitors* / Q000378:metabolism
D019440:Anti-Obesity Agents; D008024:Ligands; D017476:Receptors, Neuropeptide Y; C095889:neuropeptide Y2 receptor; C109491:neuropeptide Y4 receptor