1-Methyl-3-[di(2-thienyl)methylene]piperidine Citrateの代謝に関する研究(第2報)

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The distribution, excretion and metabolism of 1-methyl-3-[bis(2-thienyl)methylene] piperidine (I) in the rat were studied by colorimetric and radiochemical methods. It was found that I was well absorbed from the digestive tract and quickly metabolized in the liver. Immediately after the intravenous injection of tritiated I, radioactivity was the highest in the lung, relatively high in the brain, and very low in blood. Most of the radioactivity in the lung and brain was due to unchanged tritiated I, and that in the liver was due to many other radioactive metabolites. About 70% of the radio activity after the intravenous injection of tritiated I was recovered from 24 hours feces and urine, and 50% was recovered after its oral administration. Most of the radio activity in urine was due to radioactive metabolites and the amount of unchanged tritiated I and its N-demethylated compound (II) was very small. Some of the metabolites were found to be glucuronic acid conjugates but none of their aglycones were I or 3-[di(2-thienyl)methylene]piperidine hydrochloride (II). About 4% of the administered radioactivity after intraperitoneal injection of ^14C -labeled I was expired as ^<14>CO_2 in 24 hours, and most of ^<14>CO_2 was expired in the first 3 hours.
公益社団法人日本薬学会の論文
1969-03-25