4.7 Article

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

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JOURNAL OF MEDICINAL CHEMISTRY
卷 46, 期 14, 页码 2819-2822

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AMER CHEMICAL SOC
DOI: 10.1021/jm030005h

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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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