双环烷基脲促黑素聚集激素受体拮抗剂的发现：口服有效的抗肥胖疗法。

Discovery of bicycloalkyl urea melanin concentrating hormone receptor antagonists: orally efficacious antiobesity therapeutics.

作者信息

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

机构信息

Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, New Jersey 07033-0539, USA.

出版信息

J Med Chem. 2005 Apr 7;48(7):2274-7. doi: 10.1021/jm049035q.

DOI:10.1021/jm049035q

PMID:15801820

Abstract

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.

摘要

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。