赤毛猿における ^3H-cyclocytidine の分布および排泄

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The antineoplasmic agent, cyclocytidine (2, 2'-anhydro-i-β-D-arabinofurano-sylcytosine hydrochloride), was examined for distribution, excretion and metabolism in rhesus monkeys. These monkeys have a high activity of cytidine deaminase in their tissues, as well as human beings. When monkeys were injected intravenously with ^3H-cyclocytidine, high concentrations of radioactivity were detectable in the kidney, liver, pancreas and adrenal gland. The cumulative content of ^3H in the urine reached approximately 37% of the administered dose for 320 min after the injection. A very small amount of ^3H was found in the lumen of the digestive tract. It was suggested that the urinary passage might be a predominant route for the excretion of cyclocytidine. When monkeys received an oral dose of the labeled compound, the concentration of ^3H was the highest in the kidney and liver of all the organs tested, as seen in the case of intravenous injection. Orally administered ^3H-cyclocytidine underwent a metabolic destruction to ^3H-arauridine (1-β-D-arabinofuranosyluracil) through ^3H-aracytidine (1-β-D-arabinofuranosylcytosine) and finally to ^3H-water in the digestive tract. When monkeys were sacrificed 2,880 min after oral administration with ^3H-cyclocytidine, there was an increase in the relative value of this labeled compound to ^3H-aracytidine, ^3H-arauridine, and ^3H-water accompanied by the transport of the intestinal contents containing the ^3H-compounds to the anal portion. The cumulative content of urinary ^3H and the residual amount of ^3H in the digestive tract were approximately 72 and 15% of the administered dose, respectively, for the same period of exposure. This sufficient recovery of radioactivity may reflect the production of ^3H-water from the labeled compound by decomposition.
社団法人日本獣医学会の論文
1975-06-25

赤毛猿における ^3H-cyclocytidine の分布および排泄

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