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

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Absorption, excretion and metabolism of 2-amino-3-ethoxycarbonyl-6-benzyl-4,5,6,7-tetrahydrothieno [2,3-c] pyridine (Y-3642) were investigated using the radioactive compound (^<14>C-Y-3642) in mice. Excretion of radioactivity (^<14>C) was about 48% in urine, 49% in feces, within 3 days after oral administration of ^<14>C-Y-3642 at the dose of 100mg/kg. When this compound was administered intraperitoneally, the same amount of ^<14>C were excreted in urine and feces. Urinary ^<14>C was extracted with chloroform : 6-11% from alkaline urine (F-1) and 68-76% from acid urine (F-2). According to the analysis of thin-layer chromatography and inverse isotope dilution method, 17-29% of ^<14>C in F-1 was ^<14>C-Y-3642,48-59% of ^<14>C in F-2 was ^<14>C-hippuric acid, 4-6% of it was ^<14>C-benzoic acid and 1-2% of ^<14>C in the aqueous residue was ^<14>C-benzoyl glucuronide. Furthermore in the case of direct analysis of urinary ^<14>C, 0.4-1% of ^<14>C in urine was ^<14>C-Y-3642 and 42-50% was ^<14>C-hippuric acid. Unchanged ^<14>C-Y-3642 was found in the brain, but ^<14>C-benzoic acid and ^<14>C-hippuric acid mainly existed in the liver and kidney after oral administration of ^<14>C-Y-3642 in mice.
公益社団法人日本薬学会の論文
1970-03-25