Hewawasam Piyasena, Fan Wenhong, Ding Min, Flint Kim, Cook Deborah, Goggins Gregory D, Myers Robert A, Gribkoff Valentin K, Boissard Christopher G, Dworetzky Steven I, Starrett John E, Lodge Nicholas J
Department of Chemistry, The Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, Connecticut 06492, USA.
J Med Chem. 2003 Jul 3;46(14):2819-22. doi: 10.1021/jm030005h.
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.
制备了新型4-芳基-3-(羟烷基)喹啉-2-酮衍生物，并利用电生理方法对其作为非洲爪蟾卵母细胞中表达的克隆大电导钙激活钾通道hSlo的开放剂进行了评估。使用离体兔海绵体在体外研究了这些大电导钙激活钾通道开放剂对阴茎海绵体平滑肌的作用。通过这项研究，确定了一种有效的大电导钙激活钾通道开放剂可作为兔阴茎海绵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。
