抗炎症薬に関する研究(第20報)^<35>S-2-Amino-3-ethoxycarbonyl-4,5,6,7-tetrahydrothieno[2,3-c]pyridine (^<35>S-Nor-Y-3642)および^<14>C-Benzoic Acidの代謝

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The metabolic fate of 2-amino-3-ethoxycarbonyl-4,5,6,7-tetrahydrothieno[2,3-c]pyridine (Nor-Y-3642) and benzoic acid was investigated to determine the metabolic pathway of 2-amino-3-ethoxycarbonyl-6-benzyl-4,5,6,7-tetrahydrothieno[2,3-c]pyridine (Y-3642) reported in the previous paper.^<1)> When ^<35>S-Nor-Y-3642・HCl was administered intraperitoneally to mice and rats, approximately 75% of the given radioactivity was excreted as ^<35>S-Nor-Y-3642-N-glucuronide and ^<35>S-2-amino-4,5,6,7-tetrahydrothieno[2,3-c]pyridine-3-carboxylic acid (^<35>S-Nor-Y-3642-COOH) besides the unchanged compound in the urine. Furthermore, ^<35>S-2-amino-3-ethoxycarbonyl-6-acetyl-4,5,6,7-tetrahydrothieno[2,3-c]pyridine (^<35>S-N_6-Ac-Nor-Y-3642) was found as one of the metabolites of ^<35>S-Nor-Y-3642 in the bile of rats. On the other hand, when ^<14>C-benzoic acid was intraperitoneally administered to mice and rats, almost all of the given ridioactivity was excreted as ^<14>C-hippuric acid and ^<14>C-benzoyl glucuronide together with a small amount of the unchanged form in the urine. These results suggest that Nor-Y-3642 and benzoic acid are the metabolic intermediates of Y-3642 in mice and rats.
公益社団法人日本薬学会の論文
1972-09-25