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

抄録

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 (¹⁴C-Y-3642) in mice. Excretion of radioactivity (¹⁴C) was about 48% in urine, 49% in feces, within 3 days after oral administration of ¹⁴C-Y-3642 at the dose of 100mg/kg. When this compound was administered intraperitoneally, the same amount of ¹⁴C were excreted in urine and feces. Urinary ¹⁴C 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 ¹⁴C in F-1 was ¹⁴C-Y-3642, 48-59% of ¹⁴C in F-2 was ¹⁴C-hippuric acid, 4-6% of it was ¹⁴C-benzoic acid and 1-2% of ¹⁴C in the aqueous residue was ¹⁴C-benzoyl glucuronide. Furthermore in the case of direct analysis of urinary ¹⁴C, 0.4-1% of ¹⁴C in urine was ¹⁴C-Y-3642 and 42-50% was ¹⁴C-hippuric acid. Unchanged ¹⁴C-Y-3642 was found in the brain, but ¹⁴C-benzoic acid and ¹⁴C-hippuric acid mainly existed in the liver and kidney after oral administration of ¹⁴C-Y-3642 in mice.