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

• Ochi Takehiro

  Department of Immunology and Inflammation, Medicinal Biology Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.

• Fujii Takashi

  Department of Immunology and Inflammation, Medicinal Biology Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.

• Motoyama Yukio

  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.

書誌事項

タイトル別名

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

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) E₂, thromboxane (TX) B₂ and leukotriene (LT) B₄, 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 PGE₂ and TXB₂ but not LTB₄ 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 PGE₂ and TXB₂ 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

• Jpn.J.Pharmacol.

  Jpn.J.Pharmacol. 81 (1), 94-98, 1999

  公益社団法人 日本薬理学会

キーワード

• FR140423
• Yeast-induced hyperalgesia
• Prostaglandin formation
• Opioid

詳細情報

• CRID: 1390001204285452928
• NII論文ID: 10008196305
• NII書誌ID: AA00691188
• DOI: 10.1254/jjp.81.94
• COI: 1:CAS:528:DyaK1MXmt1CqurY%3D
• ISSN: 13473506
• ISSN: 00215198
• NDL書誌ID: 4867912
• PubMed: 10580376
• Web Site: https://ndlsearch.ndl.go.jp/books/R000000004-I4867912
• Web Site: https://www.jstage.jst.go.jp/article/jjp/81/1/81_1_94/_pdf
• Web Site: https://search.jamas.or.jp/link/ui/2000087879
• 本文言語コード: en
• データソース種別:
  • JaLC
  • NDL
  • Crossref
  • PubMed
  • CiNii Articles
• 抄録ライセンスフラグ: 使用不可