Author/Authors :
Hiroshi Harada، نويسنده , , Yoshimi Hirokawa، نويسنده , , Kenji Suzuki، نويسنده , , Yoichi Hiyama، نويسنده , , Mayumi Oue، نويسنده , , Hitoshi Kawashima، نويسنده , , Naoyuki Yoshida، نويسنده , , Yasuji Furutani، نويسنده , , Shiro Kato، نويسنده ,
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 and β1-AR, respectively. Furthermore, 30a showed potent agonistic activity at rat β3-AR.
