The Novel Analgesic Compound OT-7100 (5-n-Butyl-7-(3,4,5-trimethoxybenzoylamino)pyrazolo[1,5-a]pyrimidine) Attenuates Mechanical Nociceptive Responses in Animal Models of Acute and Peripheral Neuropathic Hyperalgesia

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We investigated the effects of OT-7100, a novel analgesic compound (5-<I>n</I>-butyl-7-(3, 4, 5-trimethoxybenzoylamino)pyrazolo[1, 5-<I>a</I>]pyrimidine), on prostaglandin E<SUB>2</SUB> biosynthesis in vitro, acute hyperalgesia induced by yeast and substance P in rats and hyperalgesia in rats with a chronic constriction injury to the sciatic nerve (Bennett model), which is a model for peripheral neuropathic pain. OT-7100 did not inhibit prostaglandin E<SUB>2</SUB> biosynthesis at 10<SUP>-8</SUP> - 10<SUP>-4</SUP> M. Single oral doses of 3 and 10 mg/kg OT-7100 were effective on the hyperalgesia induced by yeast. Single oral doses of 0.1, 0.3, 1 and 3 mg/kg OT-7100 were effective on the hyperalgesia induced by substance P in which indomethacin had no effect. Repeated oral administration of OT-7100 (10 and 30 mg/kg) was effective in normalizing the mechanical nociceptive threshold in the injured paw without affecting the nociceptive threshold in the uninjured paw in the Bennett model. Indomethacin had no effect in this model. While amitriptyline (10 and 30 mg/kg) and clonazepam (3 and 10 mg/kg) significantly normalized the nociceptive threshold in the injured paw, they also increased the nociceptive threshold in the uninjured paw. These results suggest that OT-7100 is a new type of analgesic with the effect of normalizing the nociceptive threshold in peripheral neuropathic hyperalgesia.

収録刊行物

  • The Japanese journal of pharmacology

    The Japanese journal of pharmacology 79(1), 65-73, 1999-01

    The Japanese Pharmacological Society

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各種コード

  • NII論文ID(NAID)
    10008194179
  • 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
    4636929
  • 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  CJP引用  NDL  J-STAGE 
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