Document Report Card

ID: ALA1145822

Journal: J Med Chem

Title: 4-Aryl-3-(hydroxyalkyl)quinolin-2-ones: novel maxi-K channel opening relaxants of corporal smooth muscle targeted for erectile dysfunction.

Authors: Hewawasam P, Fan W, Ding M, Flint K, Cook D, Goggins GD, Myers RA, Gribkoff VK, Boissard CG, Dworetzky SI, Starrett JE, Lodge NJ.

Abstract: 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.

CiteXplore: 12825925

DOI: 10.1021/jm030005h