Synthesis and Pharmacological Characterization of β2-Adrenergic Agonist Enantiomers: Zilpaterol

被引：12
|
作者：
Kern, Christopher [1 ]
Meyer, Thorsten [1 ]
Droux, Serge [3 ]
Schollmeyer, Dieter [2 ]
Miculka, Christian [1 ]
机构：
[1] Intervet Innovat GmbH, D-55270 Schwabenheim, Germany
[2] Johannes Gutenberg Univ Mainz, Inst Organ Chem, D-55099 Mainz, Germany
[3] Kiralya SAS Parc Biocitech, F-93230 Romainville, France
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 2009年 / 52卷 / 06期
关键词：
BETA-ADRENERGIC-RECEPTORS; RACTOPAMINE; SELECTIVITY; STEREOISOMERS; ANTAGONISTS; ALBUTEROL; GROWTH; ASTHMA; ASSAY;
D O I：
10.1021/jm801211c
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The beta-adrenergic agonist 1 (zilpaterol) is used as production enhancer in cattle. Binding experiments of separated enantiomers on recombinant human beta(2)-adrenergic and mu-opioid receptors and functional studies showed that the (-)-1 enantiomer accounts for essentially all the beta(2)-adrenergic agonist activity and that it exhibits less affinity toward the mu-opioid receptor than (+)-1, which is mu-opioid receptor antagonist. X-ray crystallography revealed the absolute configuration of (-)-1 to be 6R,7R.
引用
收藏
页码：1773 / 1777
页数：5
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