title: Combination of a Beta adrenoceptor modulator and a norepinephrine-serotonin uptake inhibitor for the treatment of obesity.
abstract: We report the novel combination of a selective beta adrenoceptor modulator and a norepinephrine-serotonin uptake inhibitor (sibutramine) with potential for the treatment of obesity. The synthesis and characterization of 6-[4-[2-[[(2S)-3-(9H-carbazol-4-yloxy)-2-hydroxypropyl]amino]-2-methylpropyl]phenoxy]pyridine-3-carboxamide (LY377604), a human β3-adrenergic receptor agonist and β1- and β2-adrenergic receptor antagonist with no sympathomimetic activity at the β1- and β2-adrenergic receptors, is reported. Some in vivo data in both rats and humans is presented.
authors.affiliation: Lilly Research Laboratories, Eli Lilly & Company , Lilly Corporate Center, Indianapolis, Indiana 46285, United States.
authors.forename: Cynthia D
authors.initials: CD
authors.lastname: Jesudason
authors.affiliation: Lilly Research Laboratories, Eli Lilly & Company , Lilly Corporate Center, Indianapolis, Indiana 46285, United States.
authors.forename: James E
authors.initials: JE
authors.lastname: Baker
authors.affiliation: Lilly Research Laboratories, Eli Lilly & Company , Lilly Corporate Center, Indianapolis, Indiana 46285, United States.
authors.forename: Robert D
authors.initials: RD
authors.lastname: Bryant
authors.affiliation: Lilly Research Laboratories, Eli Lilly & Company , Lilly Corporate Center, Indianapolis, Indiana 46285, United States.
authors.forename: Jack W
authors.initials: JW
authors.lastname: Fisher
authors.affiliation: Lilly Research Laboratories, Eli Lilly & Company , Lilly Corporate Center, Indianapolis, Indiana 46285, United States.
authors.forename: Libbey S
authors.initials: LS
authors.lastname: O'Farrell
authors.affiliation: Lilly Research Laboratories, Eli Lilly & Company , Lilly Corporate Center, Indianapolis, Indiana 46285, United States.
authors.forename: Gregory A
authors.initials: GA
authors.lastname: Gaich
authors.affiliation: Lilly Research Laboratories, Eli Lilly & Company , Lilly Corporate Center, Indianapolis, Indiana 46285, United States.
authors.forename: Minxia M
authors.initials: MM
authors.lastname: He
authors.affiliation: Lilly Research Laboratories, Eli Lilly & Company , Lilly Corporate Center, Indianapolis, Indiana 46285, United States.
authors.forename: Steven D
authors.initials: SD
authors.lastname: Kahl
authors.affiliation: Lilly Research Laboratories, Eli Lilly & Company , Lilly Corporate Center, Indianapolis, Indiana 46285, United States.
authors.forename: Aidas V
authors.initials: AV
authors.lastname: Kriauciunas
authors.affiliation: Lilly Research Laboratories, Eli Lilly & Company , Lilly Corporate Center, Indianapolis, Indiana 46285, United States.
authors.forename: Mark L
authors.initials: ML
authors.lastname: Heiman
authors.affiliation: Lilly Research Laboratories, Eli Lilly & Company , Lilly Corporate Center, Indianapolis, Indiana 46285, United States.
authors.forename: Mary A
authors.initials: MA
authors.lastname: Peters
authors.affiliation: Lilly Research Laboratories, Eli Lilly & Company , Lilly Corporate Center, Indianapolis, Indiana 46285, United States.
authors.forename: Christopher J
authors.initials: CJ
authors.lastname: Rito
authors.affiliation: Lilly Research Laboratories, Eli Lilly & Company , Lilly Corporate Center, Indianapolis, Indiana 46285, United States.
authors.forename: Julie H
authors.initials: JH
authors.lastname: Satterwhite
authors.affiliation: Lilly Research Laboratories, Eli Lilly & Company , Lilly Corporate Center, Indianapolis, Indiana 46285, United States.
authors.forename: Frank C
authors.initials: FC
authors.lastname: Tinsley
authors.affiliation: Lilly Research Laboratories, Eli Lilly & Company , Lilly Corporate Center, Indianapolis, Indiana 46285, United States.
authors.forename: William G
authors.initials: WG
authors.lastname: Trankle
authors.affiliation: Lilly Research Laboratories, Eli Lilly & Company , Lilly Corporate Center, Indianapolis, Indiana 46285, United States.
authors.forename: Anthony J
authors.initials: AJ
authors.lastname: Shuker
keywords: LY377604; Selective beta adrenoceptor modulator; norepinephrine-serotonin uptake inhibitor; obesity; sibutramine; β3-adrenergic receptor agonist