title: Antiinflammatory, analgesic, and antipyretic activities of methyl 7-butyl-4,5,6,7-tetrahydro-3-methylamino-4,6-dioxo-5-propyl-2H-pyrazol o[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 non-acidic agent, were examined. 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. 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. AA-2379 at 3-10 mg/kg, p.o. showed antipyretic activity in febrile rats and rabbits. 4. AA-2379, at 500 mg/kg, p.o. was not ulcerogenic in rats. 5. These data show that AA-2379 is more active than non-acidic antiinflammatory agents, such as tiaramide and aminopyrine.
authors.affiliation: Biology Laboratories, Takeda Chemical Industries, Ltd., Osaka, Japan.
authors.forename: H
authors.initials: H
authors.lastname: Makino
authors.forename: S
authors.initials: S
authors.lastname: Kuzuna
authors.forename: T
authors.initials: T
authors.lastname: Naka
authors.forename: T
authors.initials: T
authors.lastname: Saijo
authors.forename: Y
authors.initials: Y
authors.lastname: Maki
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology*; D002199:Capillary Permeability / Q000187:drug effects; D004285:Dogs; D004381:Duodenal Ulcer / Q000139:chemically induced; D004487:Edema / Q000188:drug therapy; D005260:Female; D005528:Foot; D007249:Inflammation / Q000188:drug therapy; D008297:Male; D051379:Mice; D011743:Pyrimidines / Q000494:pharmacology* / Q000633:toxicity; D011817:Rabbits; D051381:Rats; D011919:Rats, Inbred Strains
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D011743:Pyrimidines; C058395:AA 2379