Abstract
Voltage-gated sodium channels have been shown to play a critical role in neuropathic pain. With a goal to develop potent peripherally active sodium channel blockers, a series of low molecular weight biaryl substituted imidazoles, oxazoles, and thiazole carboxamides were identified with good in vitro and in vivo potency.
Copyright (c) 2010 Elsevier Ltd. All rights reserved.
MeSH terms
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Animals
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Dogs
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Humans
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Imidazoles / chemistry
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Imidazoles / metabolism
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Imidazoles / pharmacology
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Imidazoles / therapeutic use
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Microsomes, Liver / metabolism
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NAV1.7 Voltage-Gated Sodium Channel
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Neuralgia / drug therapy*
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Oxazoles / chemistry
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Oxazoles / metabolism
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Oxazoles / pharmacology
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Oxazoles / therapeutic use*
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Rats
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Sodium Channel Blockers / chemistry
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Sodium Channel Blockers / metabolism
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Sodium Channel Blockers / pharmacology
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Sodium Channel Blockers / therapeutic use*
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Sodium Channels / metabolism*
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Thiazoles / chemistry
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Thiazoles / metabolism
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Thiazoles / pharmacology
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Thiazoles / therapeutic use*
Substances
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Imidazoles
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NAV1.7 Voltage-Gated Sodium Channel
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Oxazoles
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SCN9A protein, human
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Sodium Channel Blockers
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Sodium Channels
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Thiazoles