心脈管系薬に関する研究(第8報) : 1-tert-Butylamino-3-[o-(tetrahydrofurfuryloxy)phenoxy]-2-propanol Hydrochloride(Y-6124)の代謝

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The urinary metabolites of 1-tert-butylamino-3-[o-(tetrahydrofurfuryloxy) phenoxy]-2-propanol hydrochloride (Y-6124) in rats were investigated by a radiochemical method, thin-layer chromatography (TLC), mass spectrometry, and column chromatography using Amberlite XAD-2 resin. When ^3H-labeled Y-6124 was orally administered, 84% of ^3H counts in the 24 hr urine was adsorbed by Amberlite XAD-2 resin, which was follwed by quantitative eluation with methanol. Two metabolites (I, II) were detected in the methanol eluate by TLC. These (I and II) were hydrolyzed with β-glucuronidase to the corresponding aglycones III and IV, respectively. Further, treatment of compound IV with acid afforded compound V, which was easily reverted to IV under an alkaline condition. Compound III, which was the aglycone of metabolite I, was discovered to be a monohydroxylated derivative of Y-6124 by mass spectrometry and color reactions. On the other hand, compound V, which was derived from the aglycone (IV) of metabolite II, was found to be a monohydroxylated derivative of 1-tert-butylamino-3-[o-(5-oxotetrahydrofurfuryloxy)-phenoxy]-2-propanol by the above mentioned methods. Therefore, compound IV, the aglycone of metabolite II, was considered to be a monohydroxylated derivative of 3-hydroxy-4-[o-3 (tert-butylamino-2-hydroxypropoxy) phenoxy] pentanoic acid.
社団法人日本薬学会の論文
1972-03-25