Absorption, distribution, excretion and metabolism of 2-amino-3-ethoxycarbonyl-6-benzyl-4, 5, 6, 7-tetrahydrothieno [2, 3-c] pyridine (Y-3642) were investigated using its
14C-labeled compound (
14C-Y-3642) in rats. When this compound was orally administered in a dose of 100mg/kg, radioactivity (
14C) was highly distributed in the liver, kidney, adrenals and peripheral fat. About 50% or more of
14C in the peripheral fat was extracted with chloroform its alkaline homogenate. The thin-layer chromatographic results revealed that larger amount of unchanged
14C-Y-3642 was present in the peripheral fat, a small amount in the liver and brain, but not at all in the kidney. Approximately 48% of the dose was excreted in urine and 49% in feces within 3 days after oral administration of
14C-Y-3642 (100mg/kg). Increased administration dose delayed, excretion of
14C into urine and feces, and 25% of
14C given was also excreted into bile during 24 hours. Result of thin-layer chromatography and inverse isotope dilution method of the chloro form extract showed the presence of a small amount of unchanged
14C-Y-3642 and a large amount of
14C-hippuric acid in urine, As the administered dose was increased, amount of
14C-hippuric acid excreted in urine decreased. These results clarified that
14C-Y-3642 underwent markedyl N-debenzylation in rats in vivo.
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