向精神薬に関する研究(第21報)Y-6047の生体内運命その1

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The metabolic fate of a new thienodiazepine derivative, 1-methyl-5-o-chlorophenyl-7-ethyl-1,2-dihydro-3H-thieno [2,3-e] [1,4] diazepin-2-one (Y-6047), was investigated in the rats utilizing Y-6047 labeled with ^<35>S. When this radioactive compound (^<35>S-Y-6047) was orally or intraperitoneally administered, approximately 50% of the given radioactivity (^<35>S) was excreted in the urine, most of the others in the feces, during 3 days, and 71% of the given ^<35>S was also excreted in the bile during 24 hr after oral administration. The highest concentration of ^<35>S in organs was found 0.5-1 hr after its oral administration. A high concentration of ^<35>S was present in the liver, kidney, and adrenals, and relatively low levels in the brain, peripheral fat, testes, and other tissues. Approximately 40-60% of ^<35>S in the serum was bound with serum protein. The monool and diol derivatives hydroxylated at β-position or α, β-positions of 7-ethyl group of Y-6047 were identified as the urinary metabolites of Y-6047 from their spectral data. However, all of the N_1-desmethyl, 3- or 5-phenyl hydroxy derivatives of Y-6047 and their glucuronides or sulfates, as well as the parent compound, could not be detected in the urine of drug-fed rats.
社団法人日本薬学会の論文
1973-03-25