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Synthesis and Pharmacological Characterization of b2-Adrenergic Agonist Enantiomers: Zilpaterol.

  作者 Kern, Christopher;Meyer, Thorsten;Droux, Serge;Schollmeyer, Dieter;Miculka, Christian;  
  选自 期刊  Journal of Medicinal Chemistry;  卷期  2009年52-6;  页码  1773-1777  
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[摘要]The b-adrenergic agonist 1 (zilpaterol) is used as prodn. enhancer in cattle. Binding expts. of sepd. enantiomers on recombinant human b2-adrenergic and m-opioid receptors and functional studies showed that the (-)-1 enantiomer accounts for essentially all the b2-adrenergic agonist activity and that it exhibits less affinity toward the m-opioid receptor than (+)-1, which is a m-opioid receptor antagonist. X-ray crystallog. revealed the abs. configuration of (-)-1 to be 6R,7R.

 
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