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.
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页码：2819 / 2822
页数：4
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