Abstract
A series of 1,3-diaryl 1,2,4-(4H)-triazol-5-ones was prepared and shown by electrophysiological analysis to activate a cloned maxi-K channel mSlo (or hSlo) expressed in Xenopus laevis oocytes. The effects of these structurally novel maxi-K channel openers on bladder contractile function were studied in vitro using isolated rat bladder strips pre-contracted with carbachol. Several 1,3-diaryl 1,2,4-(4H)-triazol-5-one derivatives were found to be potent smooth muscle relaxants but this activity did not completely correlate with maxi-K channel opening.
MeSH terms
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Animals
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Azo Compounds / chemical synthesis*
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Azo Compounds / pharmacology*
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Calcium / metabolism
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Carbachol / pharmacology
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Cells, Cultured / drug effects
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Electrophysiology
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Humans
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Large-Conductance Calcium-Activated Potassium Channels
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Male
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Mice
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Microinjections
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Models, Molecular
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Muscle Relaxation / drug effects
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Muscle, Smooth / physiology
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Oocytes / drug effects*
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Oocytes / physiology*
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Potassium Channels, Calcium-Activated / drug effects*
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Potassium Channels, Calcium-Activated / genetics
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Potassium Channels, Calcium-Activated / metabolism
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RNA, Messenger / metabolism
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Rats
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Structure-Activity Relationship
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Urinary Bladder / metabolism
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Urinary Incontinence / drug therapy*
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Xenopus laevis
Substances
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Azo Compounds
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Large-Conductance Calcium-Activated Potassium Channels
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Potassium Channels, Calcium-Activated
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RNA, Messenger
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Carbachol
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Calcium