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

抄録

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 ³⁵S-Nor-Y-3642·HCl was administered intraperitoneally to mice and rats, approximately 75% of the given radioactivity was excreted as ³⁵S-Nor-Y-3642-N-glucuronide and ³⁵S-2-amino-4, 5, 6, 7-tetrahydrothieno[2, 3-c]pyridine-3-carboxylic acid (³⁵S-Nor-Y-3642-COOH) besides the unchanged compound in the urine. Furthermore, ³⁵S-2-amino-3-ethoxycarbonyl-6-acetyl-4, 5, 6, 7-tetrahydrothieno[2, 3-c]pyridine (³⁵S-N₆-Ac-Nor-Y-3642) was found as one of the metabolites of ³⁵S-Nor-Y-3642 in the bile of rats. On the other hand, when ¹⁴C-benzoic acid was intraperitoneally administered to mice and rats, almost all of the given ridioactivity was excreted as ¹⁴C-hippuric acid and ¹⁴C-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.