Horie M, Baba S
Biomed Mass Spectrom. 1979 Feb;6(2):63-6. doi: 10.1002/bms.1200060205.
Metabolism of 3-phenylproply carbamate was investigated by using a stable isotope tracer technique. 3-Phenylpropanol, 3-hydroxy-3-phenylpropanol, 3-hydroxy-3-phenylpropyl carbamate, 2,3-dihydroxy-3-phenylproply carbamate, benzoic acid and hippuric acid were identified as the rat urinary metabolites. Using the dilution analysis, the amounts of metabolites in urine and faeces in rat and man were determined. In rats, 2,3-dihydroxy-3-phenylproply carbamate and 3-phenylpropanol glucuronide were excreted into the urine as the major metabolites of this drug. On the other hand, in man, the major metabolite was hippuric acid and about 30% of the administered dose was excreted as hippuric acid in the 24 h urine. The tracer technique using a singly labelled drug with carbon-13 employed in the present study provided a reliable methods for the analysis of drug metabolites and was comparable with the tracer technique using a multilabelled drug with deuterium.
采用稳定同位素示踪技术研究了3-苯基丙基氨基甲酸酯的代谢情况。3-苯基丙醇、3-羟基-3-苯基丙醇、3-羟基-3-苯基丙基氨基甲酸酯、2,3-二羟基-3-苯基丙基氨基甲酸酯、苯甲酸和马尿酸被鉴定为大鼠尿液中的代谢产物。采用稀释分析法测定了大鼠和人体尿液及粪便中代谢产物的量。在大鼠中,2,3-二羟基-3-苯基丙基氨基甲酸酯和3-苯基丙醇葡萄糖醛酸苷作为该药物的主要代谢产物排泄到尿液中。另一方面,在人体中,主要代谢产物是马尿酸,给药剂量的约30%在24小时尿液中以马尿酸形式排泄。本研究中使用单标记碳-13药物的示踪技术为药物代谢产物分析提供了一种可靠的方法,并且与使用多标记氘药物的示踪技术相当。