向精神薬に関する研究(第12報) : Y-4153の生体内運命その1

概要

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Tritium-labeled compound (^3H-Y-4153) of a new iminodibenzyl derivative, 3-chloro-5-[3-(4-piperidino-4-carbamoylpiperidino) propyl]-10,11-dihydro-5H-dibenz [b, f] azepine dihydrochloride monohydrate (Y-4153), was synthesized and its absorption, distribution, excretion and metabolism were investigated. When ^3H-Y-4153 was orally or intraperitoneally administered to rats, less than 2% of the administered radioactivity (^3H) was excreted in the urine and more than 80% of it in the feces, during 3 days. About 40% of the given ^3H was also excreted in the bile during 24 hr after oral administration. The highest concentration of ^3H in most organs was found 0.5-1 hr after its oral administration and ^3H was concentrated in the liver, adrenals and lung. Similar levels of ^3H were maintained in the brain and blood during 6 hr but their level was relatively low. More than 30% of radioactive metabolites in the bile was estimated to be a glucuronide, and three kinds of radioactive substances were extracted by the continuous extraction procedure with ethyl acetate. These radioactive substances were clarified to be the hydroxy derivatives of ^3H-Y-4153 using a thin-layer chromatography, silicagel column chromatography, color reactions and other techniques.
社団法人日本薬学会の論文
1971-10-25