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ID: ALA1136684
Journal: Bioorg Med Chem Lett
Title: Novel and potent human and rat beta3-adrenergic receptor agonists containing substituted 3-indolylalkylamines.
Authors: Harada H, Hirokawa Y, Suzuki K, Hiyama Y, Oue M, Kawashima H, Yoshida N, Furutani Y, Kato S.
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 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.
CiteXplore: 12657269