アミノピリンの代謝産物から生成するシッフの塩基によるアミノピリン, アセトアニリドおよびアモバルビタールの代謝におよぼす影響

概要

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4'-Dimethylamino-5,5'-dioxo-1,1'-diphenyl-2,2', 3-trimethyl-N-(3'-pyrazolin-3'-ylmethylidene)-3-pyrazolin-4-ylamine (Schiff's base), which was found in the urine of rats and rabbits, and in the bile of rats after the administration of aminopyrine, inhibited the activity of the enzyme metabolizing aminopyrine, acetanilide, and amobarbital in rat liver 9000×g supernatants. When Schiff's base was administered orally to rats, the metabolism of these drugs by the 9000×g supernatants of the liver was inhibited and the biological half-life of aminopyrine and amobarbital in blood of rats was lengthened. By pretreating rats with Schiff's base, the activity of these drug-metabolizing enzymes in the liver 9000×g supernatants and the ratio of liver weight to body weight increased, and the activity of glucose-6-phosphatase was inhibited. The biological half-life of aminopyrine and amobarbital in blood of rats was shortened by their pretreatment with the Schiff's base.
公益社団法人日本薬学会の論文
1976-03-25