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Bioorg Med Chem Lett. 2012 Mar 1;22(5):1903-7. doi: 10.1016/j.bmcl.2012.01.060. Epub 2012 Jan 28.

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

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  • 1Janssen Research & Development, Welsh and McKean Roads, Spring House, PA 19477-0776, USA.


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.

Copyright © 2012 Elsevier Ltd. All rights reserved.

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