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Literature DB >> 24900353

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

Cynthia D Jesudason¹, James E Baker¹, Robert D Bryant¹, Jack W Fisher¹, Libbey S O'Farrell¹, Gregory A Gaich¹, Minxia M He¹, Steven D Kahl¹, Aidas V Kriauciunas¹, Mark L Heiman¹, Mary A Peters¹, Christopher J Rito¹, Julie H Satterwhite¹, Frank C Tinsley¹, William G Trankle¹, Anthony J Shuker¹.

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.

Entities: Chemical Disease Species

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

Year: 2011 PMID： 24900353 PMCID： PMC4018109 DOI： 10.1021/ml200071k

Source DB: PubMed Journal: ACS Med Chem Lett ISSN： 1948-5875 Impact factor: 4.345

18 in total

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