Design and optimization of benzimidazole-containing transient receptor potential melastatin 8 (TRPM8) antagonists

…, RW Colburn, SK Meegalla, SK Ballentine…

Index: Parks, Daniel J.; Parsons, William H.; Colburn, Raymond W.; Meegalla, Sanath K.; Ballentine, Shelley K.; Illig, Carl R.; Qin, Ning; Liu, Yi; Hutchinson, Tasha L.; Lubin, Mary Lou; Stone, Dennis J.; Baker, Judith F.; Schneider, Craig R.; Ma, Jianya; Damiano, Bruce P.; Flores, Christopher M.; Player, Mark R. Journal of Medicinal Chemistry, 2011 , vol. 54, # 1 p. 233 - 247

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Citation Number: 45

Abstract

Transient receptor potential melastatin 8 (TRPM8) is a nonselective cation channel that is thermoresponsive to cool to cold temperatures (8− 28° C) and also may be activated by chemical agonists such as menthol and icilin. Antagonism of TRPM8 activation is currently under investigation for the treatment of painful conditions related to cold, such as cold allodynia and cold hyperalgesia. The design, synthesis, and optimization of a class of ...