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Fused tricyclic mGluR1 antagonists for the treatment of neuropathic pain

  作者 Bennett, CE; Burnett, DA; Greenlee, WJ; Knutson, CE; Korakas, P; Li, C; Tulshian, D; Wu, WL; Bertorelli, R; Fredduzzi, S; Grilli, M; Lozza, G; Reggiani, A; Veltri, A  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2012年22-4;  页码  1575-1578  
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[摘要]A series of fused tricyclic mGluR1 antagonists containing a pyridone ring were synthesized. In vitro, these antagonists were potent against both human and rat isozymes, as well as selective for inhibiting mGluR1 over mGluR5. When dosed orally, several examples were active in vivo in a rat SNL test. (C) 2012 Elsevier Ltd. All rights reserved.

 
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