Abstract
A series of imidazopyridines were evaluated as potential sodium channel blockers for the treatment of neuropathic pain. Several members were identified with good hNa(v)1.7 potency and excellent rat pharmacokinetic profiles. Compound 4 had good efficacy (52% and 41% reversal of allodynia at 2 and 4h post-dose, respectively) in the Chung rat spinal nerve ligation (SNL) model of neuropathic pain when dosed orally at 10mg/kg.
MeSH terms
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Analgesics / chemistry
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Analgesics / pharmacology
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Animals
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Inflammation / drug therapy
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Molecular Structure
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NAV1.7 Voltage-Gated Sodium Channel
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Pain / drug therapy
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Pyridines / chemistry*
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Pyridines / pharmacology*
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Rats
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Sodium Channel Blockers / chemistry*
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Sodium Channel Blockers / pharmacokinetics
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Sodium Channel Blockers / pharmacology*
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Sodium Channels / metabolism*
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Structure-Activity Relationship
Substances
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Analgesics
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NAV1.7 Voltage-Gated Sodium Channel
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Pyridines
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SCN9A protein, human
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Sodium Channel Blockers
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Sodium Channels