title: Discovery of vinylcycloalkyl-substituted benzimidazole TRPM8 antagonists effective in the treatment of cold allodynia.
abstract: 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.
authors.affiliation: Janssen Research & Development, Welsh and McKean Roads, Spring House, PA 19477-0776, USA.
authors.forename: Raul R
authors.initials: RR
authors.lastname: Calvo
authors.forename: Sanath K
authors.initials: SK
authors.lastname: Meegalla
authors.forename: Daniel J
authors.initials: DJ
authors.lastname: Parks
authors.forename: William H
authors.initials: WH
authors.lastname: Parsons
authors.forename: Shelley K
authors.initials: SK
authors.lastname: Ballentine
authors.forename: Mary Lou
authors.initials: ML
authors.lastname: Lubin
authors.forename: Craig
authors.initials: C
authors.lastname: Schneider
authors.forename: Raymond W
authors.initials: RW
authors.lastname: Colburn
authors.forename: Christopher M
authors.initials: CM
authors.lastname: Flores
authors.forename: Mark R
authors.initials: MR
authors.lastname: Player
mesh_terms: D000700:Analgesics / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D000818:Animals; D001562:Benzimidazoles / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D003080:Cold Temperature; D004285:Dogs; D057809:HEK293 Cells; D006801:Humans; D006930:Hyperalgesia / Q000188:drug therapy*; D009437:Neuralgia / Q000188:drug therapy*; D051381:Rats; D050053:TRPM Cation Channels / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D000700:Analgesics; D001562:Benzimidazoles; D050053:TRPM Cation Channels; C425966:TRPM8 protein, human; C498947:Trpm8 protein, rat; C031000:benzimidazole