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Antiinflammatory, analgesic, and antipyretic activities of methyl 7-butyl-4,5,6,7-tetrahydro-3-methylamino-4,6-dioxo-5-propyl-2H-pyrazolo[3,4-d]pyrimidine-2-carboxylate (AA-2379), a novel non-acidic agent

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Abstract

The antiinflammatory, analgesic, and antipyretic activities of methyl 7-butyl-4,5,6,7-tetrahydro-3-methylamino-4,6-dioxo-5-propyl-2H-pyrazolo[3,4-d] pyrimidine-2-carboxylate (AA-2379), a novel nonacidic agent, were examined.

  1. 1.

    AA-2379 had a potent antiinflammatory activity; 3–25 mg/kg, p.o. of the compound inhibited rat carrageenin-, bradykinin-, trypsin-, formalin-, dextran-, and nystatin-induced paw edema; mouse traumatic edema; and rat croton oil pouch inflammation by about 30%. The compound at 25–50 mg/kg, p.o. also inhibited the vascular permeability induced by histamine, serotonin, and bradykinin.

  2. 2.

    AA-2379 had an analgesic activity; the ID50 values in mouse phenylquinone-induced writhing were 10.1 mg/kg, p.o. and the compound at 12.5 mg/kg, p.o. inhibited dog urate arthritis.

  3. 3.

    AA-2379 at 3–10 mg/kg, p.o. showed antipyretic activity in febrile rats and rabbits.

  4. 4.

    AA-2379, at 500 mg/kg, p.o. was not ulcerogenic in rats.

  5. 5.

    These data show that AA-2379 is more active than non-acidic antiinflammatory agents, such as tiaramide and aminopyrine.

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Authors and Affiliations

  1. Biology Laboratories, Central Research Division, Takeda Chemical Industries, Ltd., 17-85 Jusohonmachi 2-chome, Yodogawa-ku, 532, Osaka, Japan

    H. Makino, S. Kuzuna,  T. Saijo & Y. Maki

  2. Chemistry Laboratories, Central Research Division, Takeda Chemical Industries, Ltd., 17-85 Jusohonmachi 2-chome, Yodogawa-ku, 532, Osaka, Japan

    T. Naka

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  1. H. Makino
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  2. S. Kuzuna
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  3. T. Naka
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  4. T. Saijo
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  5. Y. Maki
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Makino, H., Kuzuna, S., Naka, T. et al. Antiinflammatory, analgesic, and antipyretic activities of methyl 7-butyl-4,5,6,7-tetrahydro-3-methylamino-4,6-dioxo-5-propyl-2H-pyrazolo[3,4-d]pyrimidine-2-carboxylate (AA-2379), a novel non-acidic agent. Agents and Actions 25, 385–393 (1988). https://doi.org/10.1007/BF01965047

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  • DOI: https://doi.org/10.1007/BF01965047

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