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.
Zhu, Bin,Xia, Mingde,Xu, Xiaoqing,Ludovici, Donald W.,Tennakoon, Manomi,Youngman, Mark A.,Matthews, Jay M.,Dax, Scott L.,Colburn, Raymond W.,Qin, Ning,Hutchinson, Tasha L.,Lubin, Mary Lou,Brandt, Michael R.,Stone, Dennis J.,Flores, Christopher M.,MacIelag, Mark J.
p. 2234 - 2237
(2013/04/23)
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