アミノピリンの代謝産物とその生体内動態について

概要

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A Schiff base (4'-dimethylamino-5,5'-dioxo-1,1'-diphenyl-2,2', 3-trimethyl-N-(3'-pyrazolin-3'-ylmethylidene)-3-pyrazolin-4-ylamine) was found in the urine of rats and rabbits, and in the bile of rats as a new metabolite of aminopyrine. This Schiff base was produced by reacting 4-aminoantipyrine (AA) with 4-dimethylamino-3-formyl-2-methyl-1-phenyl-3-pyrazolin-5-one (AmCHO) in aqueous solution and in the serum of rats. When AA and AmCHO were intravenonsly administered to rats, the Schiff base was found in various tissues, urine, and bile. Therefore, it may be suggested that this metabolite (Schiff base) was excreted after being produced chemically in vivo without the enzymic reaction. When this Schiff base was orally administered to rats, it was distributed in various tissues and excreted in the bile more than in the urine.
公益社団法人日本薬学会の論文
1975-09-25