Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H- benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: Design, synthesis, and structure-activity relationships

Bioorganic and Medicinal Chemistry

Volumn 18, Issue 21, 2010, Pages 7675-7699

  Hayashi, Shigeo ^a   Nakata, Eriko ^a   Morita, Asato ^a   Mizuno, Kunihiko ^a   Yamamura, Kenzo ^a   Kato, Aki ^a   Ohashi, Katsuyo ^a  

^a PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United States)

Author keywords

GPCR; hERG potassium ion channel binding; Mechanical allodynia; Nociceptin orphanin FQ; NOP receptor selective full agonist; Peripheral spinal cord selective mechanisms; Systemically active analgesic for the treatment of neuropathic pain; 1 4 (2 Hexahydropyrrolo 3,4 c pyrrol 2(1H) yl 1H benzimidazol 1 yl) piperidin 1 yl cyclooctyl methanol (HPCOM)

Indexed keywords

[1 [4 [2 [HEXAHYDROPYRROLO[3,4 C]PYRROL 2(1H) YL] 1H BENZIMIDAZOL 1 YL]PIPERIDIN 1 YL]CYCLOOCTYL]METHANOL; NOCICEPTIN RECEPTOR; NOCICEPTIN RECEPTOR AGONIST; PIPERIDINE DERIVATIVE; UNCLASSIFIED DRUG;

ALLODYNIA; ANALGESIC ACTIVITY; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CHRONIC DISEASE; CONTROLLED STUDY; DRUG DESIGN; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; HUMAN; HUMAN CELL; MALE; NERVE COMPRESSION; NEUROPATHIC PAIN; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION;

ANALGESICS; ANIMALS; BENZIMIDAZOLES; DRUG DESIGN; DRUG EVALUATION, PRECLINICAL; HUMANS; MICROSOMES, LIVER; NEURALGIA; PYRROLES; RATS; RECEPTORS, OPIOID; STRUCTURE-ACTIVITY RELATIONSHIP;

RATTUS;

EID: 77958005386     PISSN: 09680896     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmc.2010.07.034     Document Type: Article

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