McBriar Mark D, Guzik Henry, Xu Ruo, Paruchova Jaroslava, Li Shengjian, Palani Anandan, Clader John W, Greenlee William J, Hawes Brian E, Kowalski Timothy J, O'Neill Kim, Spar Brian, Weig Blair
Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, New Jersey 07033-0539, USA.
J Med Chem. 2005 Apr 7;48(7):2274-7. doi: 10.1021/jm049035q.
Melanin concentrating hormone (MCH) is involved in regulation of food intake and energy homeostasis. Antagonists of the MCH receptor are expected to affect food intake and weight gain, making MCH-R1 an attractive target for obesity treatment. Herein, we report the discovery of a novel, orally active series of MCH-R1 antagonists that exhibit in vivo efficacy in rodent obesity models.
黑色素浓缩激素（MCH）参与食物摄入和能量平衡的调节。MCH受体拮抗剂有望影响食物摄入和体重增加，使MCH-R1成为肥胖治疗的一个有吸引力的靶点。在此，我们报告发现了一系列新型的口服活性MCH-R1拮抗剂，它们在啮齿动物肥胖模型中显示出体内疗效。
