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

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 5, 2012, Pages 1903-1907

  Calvo, Raul R ^a   Meegalla, Sanath K ^a   Parks, Daniel J ^a   Parsons, William H ^a   Ballentine, Shelley K ^a   Lubin, Mary Lou ^a   Schneider, Craig ^a   Colburn, Raymond W ^a   Flores, Christopher M ^a   Player, Mark R ^a  

^a JANSSEN RESEARCH AND DEVELOPMENT   (Belgium)

Author keywords

Benzimidazole; Cold allodynia; Cold hypersensitivity; Ion channel; Pain; Transient receptor potential melastatin; TRPM8

Indexed keywords

ANALGESIC AGENT; BENZIMIDAZOLE DERIVATIVE; CYTOCHROME P450; TRANSIENT RECEPTOR POTENTIAL CHANNEL M8; TRANSIENT RECEPTOR POTENTIAL CHANNEL M8 ANTAGONIST; UNCLASSIFIED DRUG;

ALLODYNIA; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; CELL STRAIN HEK293; COLD ALLODYNIA; COLD SENSITIVITY; COMPETITIVE INHIBITION; CONTROLLED STUDY; CYCLIZATION; DOSE RESPONSE; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG EFFICACY; DRUG HALF LIFE; HEAT SENSITIVITY; HUMAN; HUMAN CELL; HYPERSENSITIVITY; IN VITRO STUDY; LIVER MICROSOME; MAXIMUM PLASMA CONCENTRATION; NEUROPATHIC PAIN; NONHUMAN; OXIDATION REDUCTION REACTION; RAT; STRUCTURE ACTIVITY RELATION; SUBSTITUTION REACTION; SUZUKI REACTION;

ANALGESICS; ANIMALS; BENZIMIDAZOLES; COLD TEMPERATURE; DOGS; HEK293 CELLS; HUMANS; HYPERALGESIA; NEURALGIA; RATS; TRPM CATION CHANNELS;

RATTUS;

EID: 84857356525     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2012.01.060     Document Type: Article

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