1210854-16-2Relevant articles and documents
Arylglycine derivatives as potent transient receptor potential melastatin 8 (TRPM8) antagonists
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)
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.
