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Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity

  作者 SEBHAT IYASSU K; FRANKLIN CHRISTOPHER; LO MICHAEL M C; CHEN DAVID; JEWELL JAMES P; MILLER RANDY; PANG JIANMEI; PALYHA OKSANA; KAN YANQING; KELLY THERESA M; GUAN XIAOMING; MARSH DONALD J; KOSINSKI JENNIFER A; METZGER JOSEPH M; LYONS KATHRYN; DRAGOVIC JASMINKA; GUZZO PETER R; HENDERSON ALAN J; REITMAN MARC L; NARGUND RAVI P; WYVRATT MATTHEW J; LIN LINUS S  
  选自 期刊  ACS Medicinal Chemistry Letters;  卷期  2011年2-1;  页码  43-47  
  关联知识点  
 

[摘要]We report the development and characterization of compound 22 (MK-5046), a potent, selective small molecule agonist of BRS-3 (bombesin receptor subtype-3). In pharmacological testing using diet-induced obese mice, compound 22 caused mechanism-based, dose-dependent reductions in food intake and body weight.

 
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