Abstract
A series of 3-amino-1,5-benzodiazepinones were synthesized and evaluated as potential sodium channel blockers in a functional, membrane potential-based assay. One member of this series displayed subnanomolar, state-dependent sodium channel block, and was orally efficacious in a mouse model of epilepsy.
MeSH terms
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Animals
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Anticonvulsants / chemical synthesis
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Anticonvulsants / pharmacokinetics
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Anticonvulsants / pharmacology*
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Benzodiazepinones / chemical synthesis
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Benzodiazepinones / pharmacokinetics
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Benzodiazepinones / pharmacology*
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Electrophysiology
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Electroshock
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Epilepsy / drug therapy*
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Epilepsy / metabolism
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Ether-A-Go-Go Potassium Channels / antagonists & inhibitors*
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Ether-A-Go-Go Potassium Channels / metabolism
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Fluorescence Resonance Energy Transfer
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Humans
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Mice
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Molecular Structure
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Rats
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Sodium Channel Blockers / chemical synthesis
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Sodium Channel Blockers / pharmacokinetics
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Sodium Channel Blockers / pharmacology*
Substances
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Anticonvulsants
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Benzodiazepinones
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Ether-A-Go-Go Potassium Channels
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Sodium Channel Blockers