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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Author(s)

Abstract

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.

Journal

  • The Japanese Journal of Pharmacology

    The Japanese Journal of Pharmacology 79(1), 65-73, 1999-01

    The Japanese Pharmacological Society

References:  25

Cited by:  1

Codes

  • NII Article ID (NAID)
    10008194179
  • NII NACSIS-CAT ID (NCID)
    AA00691188
  • Text Lang
    ENG
  • Article Type
    Journal Article
  • ISSN
    00215198
  • NDL Article ID
    4636929
  • NDL Source Classification
    ZS51(科学技術--薬学)
  • NDL Call No.
    Z53-D199
  • Data Source
    CJP  CJPref  NDL  J-STAGE 
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