Novel and potent human and rat ??3-Adrenergic receptor agonists containing substituted 3-indolylalkylamines
摘要：
A novel series of 2-(3-indolyl)alkylamino-1-(3-chlorophenyl)ethanols was prepared and evaluated for in vitro ability to stimulate cAMP production in Chinese hamster ovary cells expressing cloned human beta(3)-AR. The optically active 30a was found to be the most potent and selective human beta(3)-AR agonist in this series with an EC(50) value of 0.062nM. In addition, 30a selectivity for human beta(3)-AR was 210-fold and 103-fold that for human beta(2)-AR and beta(1)-AR, respectively. Furthermore, 30a showed potent agonistic activity at rat beta(3)-AR.
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DOI：
10.1016/S0960-894X(03)00073-8
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年份：
2003
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来源期刊
Bioorganic & Medicinal Chemistry Letters
2003/05/01
引用走势
2004
被引量：16
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