2. Academic Validation
  3. Novel and potent human and rat beta3-adrenergic receptor agonists containing substituted 3-indolylalkylamines

Novel and potent human and rat beta3-adrenergic receptor agonists containing substituted 3-indolylalkylamines

  • Bioorg Med Chem Lett. 2003 Apr 7;13(7):1301-5. doi: 10.1016/s0960-894x(03)00073-8.
Hiroshi Harada 1,  Yoshimi Hirokawa,  Kenji Suzuki,  Yoichi Hiyama,  Mayumi Oue,  Hitoshi Kawashima,  Naoyuki Yoshida,  Yasuji Furutani,  Shiro Kato
Affiliations

Affiliation

  • 1 Chemistry Research Laboratories, Dainippon Pharmaceutical Co., Ltd., Enoki, Suita, Japan. hiroshi-harada@dainippon-pharm.co.jp
PMID: 12657269 DOI: 10.1016/s0960-894x(03)00073-8
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.

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