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Preclinical pharmacological study on ^(125)I-IPPA

         

摘要

Myocardial uptake of 125I-IPPA in rats showed a peak of 4.4% of injected dose per gram. The half elimination time of myocardium was 3.8 min and the maximal uptake of thyroid is only 0.005%ID/organ at 120min. The initial half time of 2.7 min in rabbits was obtained from the elimination curve of radioactivity in blood. In vitro binding test for 125I-IPPA to HSA showed rather constant level of activation during two hours. The second peak of extraction was observed in major organs of rats, in rabbits’ elimination of radioactivity and in binding test for 125I-IPPA to albumin in vivo. Toxicity trial was up to standard. The tolerance of a mouse to IPPA was 560 times as high as that of a person to IPPA. It demonstrated that 125I-IPPA could be quickly extracted by myocardium, and its catabolites were excreted in the urine with almost no iodine loss. All the results were found to agree with the expectations based on the principal metabolic path of phenyl fatty acid.

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