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Discovery of vinylcycloalkyl-substituted benzimidazole TRPM8 antagonists effective in the treatment of cold allodynia

RR Calvo, SK Meegalla, DJ Parks, WH Parsons…

文献索引:Calvo, Raul R.; Meegalla, Sanath K.; Parks, Daniel J.; Parsons, William H.; Ballentine, Shelley K.; Lubin, Mary Lou; Schneider, Craig; Colburn, Raymond W.; Flores, Christopher M.; Player, Mark R. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 5 p. 1903 - 1907

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被引用次数: 27

摘要

Thermosensitive transient receptor potential melastatin 8 (TRPM8) antagonists are considered to be potential therapeutic agents for the treatment of cold hypersensitivity. The discovery of a new class of TRPM8 antagonists that shows in vivo efficacy in the rat chronic constriction injury (CCI)-induced model of neuropathic pain is described.