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

页码：1773 / 1777

页数：5

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