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