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

Autor: Gregory D. Goggins, Valentin K. Gribkoff, Kim Flint, Piyasena Hewawasam, Min Ding, Steven I. Dworetzky, Nicholas J. Lodge, Wenhong Fan, Robert A. Myers, John E. Starrett, Christopher G. Boissard, Deborah A. Cook
Rok vydání: 2003
Předmět:
Zdroj: Journal of medicinal chemistry. 46(14)
ISSN: 0022-2623
Popis: 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.
Databáze: OpenAIRE