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

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

  • ACS Med Chem Lett. 2010 Oct 18;2(1):43-7. doi: 10.1021/ml100196d.
Iyassu K Sebhat 1,  Christopher Franklin 1,  Michael M-C Lo 1,  David Chen 1,  James P Jewell 1,  Randy Miller 2,  Jianmei Pang 2,  Oksana Palyha 3,  Yanqing Kan 3,  Theresa M Kelly 3,  Xiao-Ming Guan 3,  Donald J Marsh 3,  Jennifer A Kosinski 3,  Joseph M Metzger 4,  Kathryn Lyons 2,  Jasminka Dragovic 2,  Peter R Guzzo 5,  Alan J Henderson 5,  Marc L Reitman 3,  Ravi P Nargund 1,  Matthew J Wyvratt 1,  Linus S Lin 1
Affiliations

Affiliations

  • 1 Departments of Medicinal Chemistry.
  • 2 Drug Metabolism.
  • 3 Metabolic Diseases (Obesity).
  • 4 Pharmacology.
  • 5 AMRI, 26 Corporate Circle, Albany, New York 12212, United States.
PMID: 24900253 DOI: 10.1021/ml100196d
Abstract

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.

Keywords

MK-5046; bombesin receptor subtype-3 agonist; obesity.

Figures
Products