title: Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
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.
authors.affiliation: Departments of Medicinal Chemistry.
authors.forename: Iyassu K
authors.initials: IK
authors.lastname: Sebhat
authors.affiliation: Departments of Medicinal Chemistry.
authors.forename: Christopher
authors.initials: C
authors.lastname: Franklin
authors.affiliation: Departments of Medicinal Chemistry.
authors.forename: Michael M-C
authors.initials: MM
authors.lastname: Lo
authors.affiliation: Departments of Medicinal Chemistry.
authors.forename: David
authors.initials: D
authors.lastname: Chen
authors.affiliation: Departments of Medicinal Chemistry.
authors.forename: James P
authors.initials: JP
authors.lastname: Jewell
authors.affiliation: Drug Metabolism.
authors.forename: Randy
authors.initials: R
authors.lastname: Miller
authors.affiliation: Drug Metabolism.
authors.forename: Jianmei
authors.initials: J
authors.lastname: Pang
authors.affiliation: Metabolic Diseases (Obesity).
authors.forename: Oksana
authors.initials: O
authors.lastname: Palyha
authors.affiliation: Metabolic Diseases (Obesity).
authors.forename: Yanqing
authors.initials: Y
authors.lastname: Kan
authors.affiliation: Metabolic Diseases (Obesity).
authors.forename: Theresa M
authors.initials: TM
authors.lastname: Kelly
authors.affiliation: Metabolic Diseases (Obesity).
authors.forename: Xiao-Ming
authors.initials: XM
authors.lastname: Guan
authors.affiliation: Metabolic Diseases (Obesity).
authors.forename: Donald J
authors.initials: DJ
authors.lastname: Marsh
authors.affiliation: Metabolic Diseases (Obesity).
authors.forename: Jennifer A
authors.initials: JA
authors.lastname: Kosinski
authors.affiliation: Pharmacology.
authors.forename: Joseph M
authors.initials: JM
authors.lastname: Metzger
authors.affiliation: Drug Metabolism.
authors.forename: Kathryn
authors.initials: K
authors.lastname: Lyons
authors.affiliation: Drug Metabolism.
authors.forename: Jasminka
authors.initials: J
authors.lastname: Dragovic
authors.affiliation: AMRI, 26 Corporate Circle, Albany, New York 12212, United States.
authors.forename: Peter R
authors.initials: PR
authors.lastname: Guzzo
authors.affiliation: AMRI, 26 Corporate Circle, Albany, New York 12212, United States.
authors.forename: Alan J
authors.initials: AJ
authors.lastname: Henderson
authors.affiliation: Metabolic Diseases (Obesity).
authors.forename: Marc L
authors.initials: ML
authors.lastname: Reitman
authors.affiliation: Departments of Medicinal Chemistry.
authors.forename: Ravi P
authors.initials: RP
authors.lastname: Nargund
authors.affiliation: Departments of Medicinal Chemistry.
authors.forename: Matthew J
authors.initials: MJ
authors.lastname: Wyvratt
authors.affiliation: Departments of Medicinal Chemistry.
authors.forename: Linus S
authors.initials: LS
authors.lastname: Lin
keywords: MK-5046; bombesin receptor subtype-3 agonist; obesity