Absorption, distribution, excretion, and metabolism of 1-(5-oxohexyl)theobromine (BL 191) in rats.

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The absorption, distribution, and urinary excretion of 1-(5-oxohexyl) theobromine (BL 191) after oral administration (400 mg/kg) or intravenous injection (25 mg/kg) were studied in rats, using thin-layer chromatography and colorimetry. At the same time, identification of the chemical structure on 4 metabolites of BL 191 in the urine was made. Plasma BL 191 levels reached a maximum within 10 min-1 hr after the oral administration and declined linearly thereafter. BL 191 was no longer detected in plasma 24 hr after the administration. After the intravenous administration, BL 191 was rapidly eliminated from plasma and could not be found 6 hr after the administration. The experiment in rats with the ligated pylorus revealed that a considerable amount of BL 191 administered was absorbed from the stomach as well as from the duodenum and the small intestine after the oral administration. In the organs like the brain, heart, liver, lung, and kidney and the skeletal muscle examined, BL 191 was found to approximately the same extent 10 min after the oral administration and showed the time-course similar to that of plasma levels. BL 191 and its metabolites were rapidly excreted largely in the urine. The total amount excreted in the urine was 1.3% and 68.3% of the dose administered as unchanged BL 191 and as the metabolites, respectively, and most of the excretion was carried out within 24 hr after the administration. 1-(4, 5-Dihydroxyhexyl) theobromine and 1-(3-carboxypropyl) theobromine were main urinary metabolites of BL 191.

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