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

Autor: Hewawasam P; Department of Chemistry, The Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, Connecticut 06492, USA. hewawasp@bms.com, Fan W, Ding M, Flint K, Cook D, Goggins GD, Myers RA, Gribkoff VK, Boissard CG, Dworetzky SI, Starrett JE Jr, Lodge NJ
Jazyk: angličtina
Zdroj: Journal of medicinal chemistry [J Med Chem] 2003 Jul 03; Vol. 46 (14), pp. 2819-22.
DOI: 10.1021/jm030005h
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.
Databáze: MEDLINE