4-Aryl-3-(hydroxyalkyl)quinolin-2-ones:  Novel Maxi-K Channel Opening Relaxants of Corporal Smooth Muscle Targeted for Erectile Dysfunction

Autor: Hewawasam, P., Fan, W., Ding, M., Flint, K., Cook, D., Goggins, G. D., Myers, R. A., Gribkoff, V. K., Boissard, C. G., Dworetzky, S. I., Starrett, J. E., Jr., Lodge, N. J.
Zdroj: Journal of Medicinal Chemistry; July 2003, Vol. 46 Issue: 14 p2819-2822, 4p
Abstrakt: 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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