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Imidazopyridines: a novel class of hNav1.7 channel blockers.
London, Clare; Hoyt, Scott B; Parsons, William H; Williams, Brande S; Warren, Vivien A; Tschirret-Guth, Richard; Smith, McHardy M; Priest, Birgit T; McGowan, Erin; Martin, William J; Lyons, Kathryn A; Li, Xiaohua; Karanam, Bindhu V; Jochnowitz, Nina; Garcia, Maria L; Felix, John P; Dean, Brian; Abbadie, Catherine; Kaczorowski, Gregory J; Duffy, Joseph L.
Afiliación
  • London C; Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. clare_london@merck.com
Bioorg Med Chem Lett ; 18(5): 1696-701, 2008 Mar 01.
Article en En | MEDLINE | ID: mdl-18243692
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.
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Texto completo: 1 Bases de datos: MEDLINE Asunto principal: Piridinas / Canales de Sodio / Bloqueadores de los Canales de Sodio Límite: Animals Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2008 Tipo del documento: Article País de afiliación: Estados Unidos
Texto completo
Imprimir
XML
PubMed Links
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Texto completo: 1 Bases de datos: MEDLINE Asunto principal: Piridinas / Canales de Sodio / Bloqueadores de los Canales de Sodio Límite: Animals Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2008 Tipo del documento: Article País de afiliación: Estados Unidos