Abstract
Novel cyclohexadienes have been identified as potent and specific IK(Ca)-channel blockers. In this communication we describe their synthesis as well as their chemical and biological properties. A selected derivative is being enriched in rat brain and reduces the infarct volume, intracranial pressure as well as the water content in a rat subdural hematoma model of traumatic brain injury after iv administration.
MeSH terms
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Animals
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Body Water / drug effects*
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Body Water / metabolism
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Brain Infarction / drug therapy
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Brain Injuries / drug therapy
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Cyclohexanes / chemical synthesis
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Cyclohexanes / pharmacology*
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Cyclohexenes
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Disease Models, Animal
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Hematoma, Subdural / drug therapy
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Intermediate-Conductance Calcium-Activated Potassium Channels
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Intracranial Pressure / drug effects*
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Potassium Channel Blockers / chemical synthesis
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Potassium Channel Blockers / pharmacology*
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Potassium Channels / metabolism*
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Rats
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Structure-Activity Relationship
Substances
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Cyclohexanes
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Cyclohexenes
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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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1,4-cyclohexadiene