Novel and potent human and rat β 3-Adrenergic receptor agonists containing substituted 3-indolylalkylamines

H Harada, Y Hirokawa, K Suzuki, Y Hiyama…

Index: Harada, Hiroshi; Hirokawa, Yoshimi; Suzuki, Kenji; Hiyama, Yoichi; Oue, Mayumi; Kawashima, Hitoshi; Yoshida, Naoyuki; Furutani, Yasuji; Kato, Shiro Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 7 p. 1301 - 1305

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Citation Number: 50

Abstract

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 β3-AR. The optically active 30a was found to be the most potent and selective human β3-AR agonist in this series with an EC50 value of 0.062 nM. In addition, 30a selectivity for human β3-AR was 210-fold and 103-fold that for human β2-AR ...