4-Aryl-3-(mercapto)quinolin-2-ones: novel maxi-K channel opening relaxants of corporal smooth muscle.
A novel series of 4-aryl-3-(mercapto)quinolin-2-one derivatives was 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. In vivo efficacy has been demonstrated with a selective maxi-K opening relaxant in a rat model of erectile function.
Hewawasam
Piyasena
P
Department of Chemistry, The Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA. hewawasp@bms.com
Fan
Wenhong
W
Cook
Deborah A
DA
Newberry
Kimberly S
KS
Boissard
Christopher G
CG
Gribkoff
Valentin K
VK
Starrett
John
J
Lodge
Nicholas J
NJ
D000818:Animals; D005260:Female; D066298:In Vitro Techniques; D051036:Large-Conductance Calcium-Activated Potassium Channels; D008297:Male; D009131:Muscle, Smooth, Vascular / Q000187:drug effects* / Q000502:physiology; D010413:Penis / Q000187:drug effects* / Q000502:physiology; D024681:Potassium Channels, Calcium-Activated / Q000502:physiology*; D015363:Quinolones / Q000737:chemistry* / Q000494:pharmacology; D011817:Rabbits; D051381:Rats; D011916:Rats, Inbred F344; D014664:Vasodilation / Q000187:drug effects* / Q000502:physiology; D014982:Xenopus laevis
D051036:Large-Conductance Calcium-Activated Potassium Channels; D024681:Potassium Channels, Calcium-Activated; D015363:Quinolones