Abstract
4-Phenyl-4H-pyrans have been identified as potent and specific IK(Ca) channel blockers. Their synthesis and structure-activity relationships are described. A selected derivative, rac-11, reduces the infarct volume in a rat subdural hematoma model of traumatic brain injury after iv administration.
MeSH terms
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Animals
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Blood Pressure
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Brain / metabolism
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Brain / pathology
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Brain Infarction / drug therapy
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Brain Injuries / drug therapy
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Disease Models, Animal
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Dose-Response Relationship, Drug
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Heart Rate
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Hematoma, Subdural / drug therapy
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Hematoma, Subdural / pathology
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Intermediate-Conductance Calcium-Activated Potassium Channels
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Nifedipine / analogs & derivatives
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Nifedipine / pharmacology
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Potassium Channel Blockers / administration & dosage
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Potassium Channel Blockers / chemical synthesis*
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Potassium Channel Blockers / pharmacology
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Potassium Channels / drug effects*
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Potassium Channels / metabolism
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Pyrans / administration & dosage
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Pyrans / chemical synthesis*
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Pyrans / pharmacology
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Rats
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Structure-Activity Relationship
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Time Factors
Substances
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Intermediate-Conductance Calcium-Activated Potassium Channels
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Kcnn4 protein, rat
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Potassium Channel Blockers
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Potassium Channels
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Pyrans
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Nifedipine