2. Academic Validation
  3. Combination of a Beta adrenoceptor modulator and a norepinephrine-serotonin uptake inhibitor for the treatment of obesity

Combination of a Beta adrenoceptor modulator and a norepinephrine-serotonin uptake inhibitor for the treatment of obesity

  • ACS Med Chem Lett. 2011 May 23;2(8):583-6. doi: 10.1021/ml200071k.
Cynthia D Jesudason 1,  James E Baker 1,  Robert D Bryant 1,  Jack W Fisher 1,  Libbey S O'Farrell 1,  Gregory A Gaich 1,  Minxia M He 1,  Steven D Kahl 1,  Aidas V Kriauciunas 1,  Mark L Heiman 1,  Mary A Peters 1,  Christopher J Rito 1,  Julie H Satterwhite 1,  Frank C Tinsley 1,  William G Trankle 1,  Anthony J Shuker 1
Affiliations

Affiliation

  • 1 Lilly Research Laboratories, Eli Lilly & Company , Lilly Corporate Center, Indianapolis, Indiana 46285, United States.
PMID: 24900353 DOI: 10.1021/ml200071k
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.

Keywords

LY377604; Selective beta adrenoceptor modulator; norepinephrine-serotonin uptake inhibitor; obesity; sibutramine; β3-adrenergic receptor agonist.

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