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Updated: May 14, 2026

A Simple and Inexpensive Method for Determining Cold Sensitivity and Adaptation in Mice
Published on: March 17, 2015
Arylglycine derivatives as potent transient receptor potential melastatin 8 (TRPM8) antagonists
Bin Zhu1, Mingde Xia, Xiaoqing Xu
1Janssen Research & Development, L.L.C., Welsh & McKean Roads, Spring House, PA 19477, USA. bzhu@its.jnj.com
Abstract:
A series of arylglycine-based analogs was synthesized and tested for TRPM8 antagonism in a cell-based functional assay. Following structure-activity relationship studies in vitro, a number of compounds were identified as potent TRPM8 antagonists and were subsequently evaluated in an in vivo pharmacodynamic assay of icilin-induced 'wet-dog' shaking in which compound 12 was fully effective. TRPM8 antagonists of the type described here may be useful in treating pain conditions wherein cold hypersensitivity is a dominant feature.
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