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4-aryl-3-(mercapto)quinolin-2-ones: novel maxi-K channel opening relaxants of corporal smooth muscle

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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 14, 期 17, 页码 4479-4482

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2004.06.051

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A novel series of 4-aryl-3-(mercapto)quinolin-2-one derivatives was 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. In vivo efficacy has been demonstrated with a selective maxi-K opening relaxant in a rat model of erectile function. (C) 2004 Elsevier Ltd. All rights reserved.

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