4-aryl-3-(hydroxyalkyl)quinolin-2-ones: Novel maxi-K channel opening relaxants of corporal smooth muscle targeted for erectile dysfunction

被引：90

作者：

Hewawasam, P

Fan, WH

Ding, M

Flint, M

Cook, D

Goggins, GD

Myers, RA

Gribkoff, VK

Boissard, CG

Dworetzky, SI

Starrett, JE

Lodge, NJ

机构：

[1] Bristol Myers Squibb Co, Pharmaceut Res Inst, Dept Chem, Wallingford, CT 06492 USA

[2] Bristol Myers Squibb Co, Pharmaceut Res Inst, Dept Neurosci Genitourinary Drug Discovery, Wallingford, CT 06492 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2003年 / 46卷 / 14期

关键词：

D O I：

10.1021/jm030005h

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Novel 4-aryl-3-(hydroxyalkyl)quinoline-2-one derivatives were prepared and evaluated as openers of the cloned maxi-K channel hSlo expressed in Xenopus laevis oocytes by utilizing electrophysiological methods. The effect of these maxi-K openers on corporal smooth muscle was studied in vitro using isolated rabbit corpus cavernosum. From this study, a potent maxi-K opener was identified as an effective relaxant of rabbit corporal smooth muscle and shown to be active in an in vivo animal model of male erectile function.

引用

页码：2819 / 2822

页数：4

共 21 条

[1] PHYSIOLOGY OF PENILE ERECTION [J].