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

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. 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. 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. AA-2379 at 3–10 mg/kg, p.o. showed antipyretic activity in febrile rats and rabbits. AA-2379, at 500 mg/kg, p.o. was not ulcerogenic in rats. These data show that AA-2379 is more active than non-acidic antiinflammatory agents, such as tiaramide and aminopyrine.