抗炎症薬に関する研究(第7報) : 2-Amino-3-ethoxycarbonyl-6-benzyl(α-^<14>C)-4,5,6,7-tetrahydrothieno[2,3-c]pyridine(^<14>C-Y-3642)のラットにおける吸収, 生体内分布, 排泄および代謝

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Absorption, distribution, excretion and metabolism of 2-amino-3-ethoxycarbonyl-6-benzyl-4,5,6,7-tetrahydrothieno [2,3-c] pyridine (Y-3642) were investigated using its ^<14>C-labeled compound (^<14>C-Y-3642) in rats. When this compound was orally administered in a dose of 100mg/kg, radioactivity (^<14>C) was highly distributed in the liver, kidney, adrenals and peripheral fat. About 50% or more of ^<14>C in the peripheral fat was extracted with chloroform its alkaline homogenate. The thin-layer chromatographic results revealed that larger amount of unchanged ^<14>C-Y-3642 was present in the peripheral fat, a small amount in the liver and brain, but not at all in the kidney. Approximately 48% of the dose was excreted in urine and 49% in feces within 3 days after oral administration of ^<14>C-Y-3642 (100mg/kg). Increased administration dose delayed, excretion of ^<14>C into urine and feces, and 25% of ^<14>C given was also excreted into bile during 24 hours. Result of thin-layer chromatography and inverse isotope dilution method of the chloro form extract showed the presence of a small amount of unchanged ^<14>C-Y-3642 and a large amount of ^<14>C-hippuric acid in urine, As the administered dose was increased, amount of ^<14>C-hippuric acid excreted in urine decreased. These results clarified that ^<14>C-Y-3642 underwent markedyl N-debenzylation in rats in vivo.
公益社団法人日本薬学会の論文
1970-03-25