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ACS Med Chem Lett. 2011 May 23;2(8):583-6. doi: 10.1021/ml200071k. eCollection 2011 Aug 11.

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

Author information

1
Lilly Research Laboratories, Eli Lilly & Company , Lilly Corporate Center, Indianapolis, Indiana 46285, United States.

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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