The Profile of FR140423, a Novel Anti-inflammatory Compound, in Yeast-Induced Rat Hyperalgesia

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著者

    • Ochi Takehiro OCHI Takehiro
    • Department of Immunology and Inflammation, Medicinal Biology Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
    • Fujii Takashi FUJII Takashi
    • Department of Immunology and Inflammation, Medicinal Biology Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
    • GOTO Toshio
    • Department of Immunology and Inflammation, Medicinal Biology Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.

抄録

The mechanism of action of FR140423 (3-(difluoromethyl)-1-(4-methoxyphenyl)-5-[4-(methylsulfinyl)phenyl]pyrazole), a novel anti-inflammatory compound, in a rat yeast-induced hyperalgesic model was investigated and compared with those of indomethacin and morphine. We tested the inhibitory effects of FR140423 on the formation of arachidonic acid metabolites, prostaglandin (PG) E<SUB>2</SUB>, thromboxane (TX) B<SUB>2</SUB> and leukotriene (LT) B<SUB>4</SUB>, in yeast-injected inflamed paws and the effect of the opioid receptor antagonist naloxone on FR140423-induced anti-hyperalgesic effect and inhibition of the formation of arachidonic acid metabolites. Oral administration of FR140423 showed a dose-dependent anti-hyperalgesic effect. This effect was fourfold more potent than that of indomethacin but less potent than that of morphine. Unlike morphine, FR140423 suppressed the levels of PGE<SUB>2</SUB> and TXB<SUB>2</SUB> but not LTB<SUB>4</SUB> in inflamed paws. FR140423 did not inhibit yeast-induced paw edema. The anti-hyperalgesic effect of FR140423 in yeast-injected rat paws was partially blocked by naloxone. However, the inhibitory effects of FR140423 on the formation of PGE<SUB>2</SUB> and TXB<SUB>2</SUB> in yeast-injected rat paws were not antagonized by naloxone. These results suggest that FR140423 shows a potent anti-hyperalgesic effect mediated by inhibition of PGs in inflamed tissue and by activation of opioid receptors.

収録刊行物

  • The Japanese journal of pharmacology

    The Japanese journal of pharmacology 81(1), 94-98, 1999-09

    The Japanese Pharmacological Society

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各種コード

  • NII論文ID(NAID)
    10008196305
  • NII書誌ID(NCID)
    AA00691188
  • 本文言語コード
    ENG
  • 資料種別
    ART
  • ISSN
    00215198
  • NDL 記事登録ID
    4867912
  • NDL 雑誌分類
    ZS51(科学技術--薬学)
  • NDL 請求記号
    Z53-D199
  • データ提供元
    CJP書誌  NDL  J-STAGE 
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