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

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)-induc...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2012-03, Vol.22 (5), p.1903-1907
Hauptverfasser:	Calvo, Raul R., Meegalla, Sanath K., Parks, Daniel J., Parsons, William H., Ballentine, Shelley K., Lubin, Mary Lou, Schneider, Craig, Colburn, Raymond W., Flores, Christopher M., Player, Mark R.
Format:	Artikel
Sprache:	eng
Schlagworte:	Analgesics - chemistry Analgesics - pharmacokinetics Analgesics - pharmacology Analgesics - therapeutic use Animals antagonists Benzimidazole Benzimidazoles - chemistry Benzimidazoles - pharmacokinetics Benzimidazoles - pharmacology Benzimidazoles - therapeutic use Biological and medical sciences chemistry Cold allodynia Cold hypersensitivity Cold Temperature cold treatment Dogs HEK293 Cells Humans Hyperalgesia - drug therapy hypersensitivity Ion channel Medical sciences Neuralgia - drug therapy Pain Pharmacology. Drug treatments Rats Transient receptor potential melastatin TRPM Cation Channels - antagonists & inhibitors TRPM Cation Channels - metabolism TRPM8
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Zusammenfassung:	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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2012.01.060