Abstract
A series of benzazepinones were synthesized and evaluated as hNa(v)1.7 sodium channel blockers. Several compounds from this series displayed good oral bioavailability and exposure and were efficacious in a rat model of neuropathic pain.
MeSH terms
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Animals
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Benzodiazepinones / chemical synthesis*
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Benzodiazepinones / pharmacokinetics
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Benzodiazepinones / therapeutic use*
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Biological Availability
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Disease Models, Animal
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Dogs
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Drug Evaluation, Preclinical
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Molecular Structure
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NAV1.7 Voltage-Gated Sodium Channel
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Neuralgia / drug therapy*
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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 / therapeutic use*
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Sodium Channels / chemistry
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Sodium Channels / drug effects*
Substances
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Benzodiazepinones
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NAV1.7 Voltage-Gated Sodium Channel
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Scn9a protein, rat
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Sodium Channel Blockers
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Sodium Channels