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J Med Chem ; 46(14): 2819-22, 2003 Jul 03.
Article in English | MEDLINE | ID: mdl-12825925

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.


Subject(s)
Muscle, Smooth/drug effects , Penis/drug effects , Potassium Channels, Calcium-Activated/drug effects , Quinolones/chemical synthesis , Animals , Blood Pressure/drug effects , Electric Stimulation , Erectile Dysfunction/drug therapy , In Vitro Techniques , Large-Conductance Calcium-Activated Potassium Channels , Male , Muscle Relaxation/drug effects , Muscle, Smooth/physiology , Penile Erection/drug effects , Penis/innervation , Penis/physiology , Pressure , Quinolones/chemistry , Quinolones/pharmacology , Rabbits , Rats , Rats, Inbred F344 , Structure-Activity Relationship
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