Identification, kinetic and quantitative study of [2-14C] and [1-Me-14C]caffeine metabolites in rat's urine by chromatographic separations

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Abstract

The urinary metabolites of [2-14C] and [1-Me-14C]caffeine administered orally have been separated by two-dimensional thin-layer chromatography from whole urine, and localized by autoradiography.

The scanning of chromatograms gives quantitative results showing the importance of the metabolic pathway leading to trimethyldihydrouric acid. The following three new metabolites were identified in rat's urine: 1,7-dimethyluric, N-methylurea, and NN′-dimethylurea.

The excretion kinetics of each metabolite show that caffeine, theophylline, trimethylallantoin, and an unknown derivative which is either an isomer or a precursor of trimethylallantoin were excreted later than the other metabolites as a whole.

References (7)

  • K.L. Khanna et al.

    Toxicol. Appl. Pharmacol.

    (1972)
  • A.W. Burg et al.

    Biochem. Pharmacol.

    (1972)
  • F. Bergmann et al.

    J. Biol. Chem.

    (1956)
There are more references available in the full text version of this article.

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