| Autor: |
Harada H; Chemistry Research Laboratories, Dainippon Pharmaceutical Co., Ltd., Enoki, Suita, Japan. hiroshi-harada@dainippon-pharm.co.jp, Hirokawa Y, Suzuki K, Hiyama Y, Oue M, Kawashima H, Yoshida N, Furutani Y, Kato S |
| Jazyk: |
angličtina |
| Zdroj: |
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2003 Apr 07; Vol. 13 (7), pp. 1301-5. |
| DOI: |
10.1016/s0960-894x(03)00073-8 |
| Abstrakt: |
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. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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