Kowalski Timothy J, Sasikumar Thavalakulamgar
Department of CV/Metabolic Diseases, Schering-Plough Research Institute, Kenilworth, New Jersey 07033, USA.
BioDrugs. 2007;21(5):311-21. doi: 10.2165/00063030-200721050-00003.
There is compelling genetic and pharmacologic evidence to indicate that melanin-concentrating hormone receptor-1 (MCHR1) signaling is involved in the regulation of food intake and energy expenditure. The medical need for novel therapies to treat obesity and related metabolic disorders has led to a great deal of interest by pharmaceutical companies in the discovery of MCHR1 antagonists. Recent publications describing preclinical studies have demonstrated that small-molecule MCHR1 antagonists decrease food intake, bodyweight, and adiposity in rodent models of obesity. Results from ongoing early-stage clinical trials with MCHR1 antagonists are eagerly awaited, as is the movement of other MCHR1 antagonists into the clinic.
有令人信服的遗传学和药理学证据表明，黑色素浓缩激素受体1（MCHR1）信号传导参与食物摄入和能量消耗的调节。治疗肥胖症及相关代谢紊乱的新型疗法的医学需求，引发了制药公司对发现MCHR1拮抗剂的浓厚兴趣。最近描述临床前研究的出版物表明，小分子MCHR1拮抗剂可降低肥胖啮齿动物模型的食物摄入量、体重和肥胖程度。人们急切期待MCHR1拮抗剂正在进行的早期临床试验结果，以及其他MCHR1拮抗剂进入临床阶段的进展。
