Harada Hiroshi, Hirokawa Yoshimi, Suzuki Kenji, Hiyama Yoichi, Oue Mayumi, Kawashima Hitoshi, Yoshida Naoyuki, Furutani Yasuji, Kato Shiro
Chemistry Research Laboratories, Dainippon Pharmaceutical Co., Ltd., Enoki, Suita, Japan.
Bioorg Med Chem Lett. 2003 Apr 7;13(7):1301-5. doi: 10.1016/s0960-894x(03)00073-8.
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.
