首页> 外文期刊>Journal of Medicinal Chemistry >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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4-Aryl-3-(hydroxyalkyl)quinolin-2-ones: Novel Maxi-K Channel Opening Relaxants of Corporal Smooth Muscle Targeted for Erectile Dysfunction

机译:4-芳基-3-(羟烷基)喹啉-2-酮:针对勃起功能障碍的新型体壁平滑肌Maxi-K通道开放松弛剂

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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.
机译:制备了新的4-芳基-3-(羟烷基)喹啉-2-酮衍生物,并利用电生理方法评价了在非洲爪蟾卵母细胞中表达的克隆的maxi-K通道hSlo的开放性。使用离体兔海绵体在体外研究了这些maxi-K开环剂对体平滑肌的作用。从这项研究中,有效的maxi-K开环剂被鉴定为兔体平滑肌的有效松弛剂,并在雄性勃起功能的体内动物模型中显示出活性。

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