Journal article
4-Aryl-3-(hydroxyalkyl)quinolin-2-ones: Novel Maxi-K Channel Opening Relaxants of Corporal Smooth Muscle Targeted for Erectile Dysfunction
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 …
Authors
Hewawasam P; Fan W; Ding M; Flint K; Cook D; Goggins GD; Myers RA; Gribkoff VK; Boissard CG; Dworetzky SI
Journal
Journal of Medicinal Chemistry, Vol. 46, No. 14, pp. 2819–2822
Publisher
American Chemical Society (ACS)
Publication Date
July 1, 2003
DOI
10.1021/jm030005h
ISSN
0022-2623
Associated Experts
Fields of Research (FoR)
Medical Subject Headings (MeSH)
AnimalsBlood PressureElectric StimulationErectile DysfunctionIn Vitro TechniquesLarge-Conductance Calcium-Activated Potassium ChannelsMaleMuscle RelaxationMuscle, SmoothPenile ErectionPenisPotassium Channels, Calcium-ActivatedPressureQuinolonesRabbitsRatsRats, Inbred F344Structure-Activity Relationship