Synthesis of a novel 6,14-epoxymorphinan derivative and its pharmacology

Bioorganic and Medicinal Chemistry Letters

Volumn 18, Issue 24, 2008, Pages 6398-6401

  Nemoto, Toru ^a   Fujii, Hideaki ^a   Narita, Minoru ^b   Miyoshi, Kan ^b   Nakamura, Atsushi ^b   Suzuki, Tsutomu ^b   Nagase, Hiroshi ^a  

^a KITASATO UNIVERSITY   (Japan)

^b HOSHI UNIVERSITY   (Japan)

Author keywords

6,14 Epoxymorphinan; Analgesics; Naltrexone; Opioid

Indexed keywords

6,14 EPOXYMORPHINAN DERIVATIVE; BENZAMIDE DERIVATIVE; KAPPA OPIATE RECEPTOR; KAPPA OPIATE RECEPTOR AGONIST; MORPHINAN DERIVATIVE; NALFURAFINE; NS 22; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTINOCICEPTION; ARTICLE; BINDING ASSAY; DRUG ACTIVITY; DRUG DESIGN; DRUG RECEPTOR BINDING; DRUG SYNTHESIS; HOT PLATE TEST; MOUSE; NONHUMAN; STRUCTURE ACTIVITY RELATION; TAIL FLICK TEST;

ANALGESICS; ANIMALS; BENZAMIDES; CHEMISTRY, PHARMACEUTICAL; DRUG DESIGN; GUANOSINE 5'-O-(3-THIOTRIPHOSPHATE); HYDROGEN BONDING; INJECTIONS, SUBCUTANEOUS; IONS; LIGANDS; MICE; MODELS, BIOLOGICAL; MODELS, CHEMICAL; MORPHINANS; PROTEIN BINDING; RECEPTORS, OPIOID, KAPPA;

MUS;

EID: 56249107674     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.10.081     Document Type: Article

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17. Assessment of antinociception: To prevent tissue damage, we established a 30 s (hot-plate test) or 10 s (tail-flick test) cut-off time. Each animal served as its own control, and the latency to response was measured both before and after drug administration. Antinociception was calculated as percentage of antinociception according to the following formula: % antinociception = (test latency - pre-drug latency)/(cut-off time - pre-drug latency) × 100. Antinociceptive response represents as the mean ± SEM of % antinociception.