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-N
6-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.
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