Metabolic Fate of Urokinase

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The metabolic fate of ^<131>I-urokinase in rats and dogs was investigated. The radioactivity in the blood of both animals after intravenous administration rapidly decreased in early stage, followed by a slow decrease of the radioactivity. When ^<131>I-urokinase was given into rats by intravenous infusion, the peak of radioactivity in the blood was found at the end of the dosing period. The radioactivity in the liver and kidneys of the rats 15 min after intravenous administration of ^<131>I-urokinase was found to be 43 and 32% of the administered radioactivity, respectively. In the rats approximately 80% of the administered radioactivity was recovered, mainly in the urine in 3 days. The radioactivity derived from high-molecular compounds in the serum of rats receiving ^<131>I-urokinase intravenously was approximately 95% of the radioactivity detected 1 min after dosing, 70% at 20 min and 40% at 60 min. An artificial thrombus was prepared by the method of Chandler and radioactivity of the thrombus was determined by incubating with radioiodinated urokinase, plasminogen, plasmin or reference compounds. After a 6 hr incubation the ratio of the radioactivity concentration of the thrombus (cpm/mg) to that of the blood (cpm/mg) was 2 for ^<131>I-urokinase, 3 for ^<131>I-plasminogen, 3 for ^<131>I-plasmin, 0.7 for ^<131>I-human serum albumin and 0.8 for Na^<131>I. When the blood added with ^<131>I-plasminogen was employed for the preparation of an artificial thrombus, approximately 15% of the added radioactivity was detected in the thrombus.
公益社団法人日本薬学会の論文
1974-04-25

Metabolic Fate of Urokinase

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