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I-纤维蛋白原作为一种亲肿瘤放射性诊断剂:荷瘤小鼠体内的分布动力学

I-fibrinogen as an oncophilic radiodiagnostic agent: distribution kinetics in tumour-bearing mice.

作者信息

Krohn K A, DeNardo S J, Wheeler D W, DeNardo G L

出版信息

Br J Cancer. 1977 Aug;36(2):227-34. doi: 10.1038/bjc.1977.182.

Abstract

Fibrinogen radioiodinated by the iodine monochloride method was tested as a tumour radiodiagnostic agent in mice. The I-fibrinogen cleared from the blood of tumour-bearing mice more rapidly than from that of normal mice, but it cleared from the whole body more slowly, suggesting it accumulated in a substantial tumour-related compartment in the abnormal mice. The tumour concentration steadily increased for 4 h after injection, at which time it reached a peak concentration of 11-4% of the injected dose/g. This concentration was higher than the peak concentration for Ga-citrate (not reached until 24 h) or any other oncophilic radiopharmaceutical tested in this tumour model. The early accumulation is consistent with the use of 123I as a tracer label for fibrinogen. A combination of the large tumour concentration of I-fibrinogen, an increased catabolic rate induced by chemical modification, and the exceptional nuclear properties of 123I for scintigraphic imaging, could lead to a very useful radiodiagnostic procedure for cancer.

摘要

用一氯化碘法放射性碘化的纤维蛋白原在小鼠体内作为肿瘤放射性诊断剂进行了测试。与正常小鼠相比,荷瘤小鼠血液中清除的碘 - 纤维蛋白原更快,但从全身清除得更慢,这表明它在异常小鼠体内大量积聚在与肿瘤相关的区室中。注射后4小时肿瘤浓度持续升高,此时达到峰值浓度,为注射剂量/克的11 - 4%。该浓度高于柠檬酸镓(直到24小时才达到峰值)或在此肿瘤模型中测试的任何其他亲肿瘤放射性药物的峰值浓度。早期积聚与将123I用作纤维蛋白原的示踪标记一致。碘 - 纤维蛋白原在肿瘤中的高浓度、化学修饰诱导的分解代谢率增加以及123I用于闪烁成像的特殊核特性相结合,可能会产生一种非常有用的癌症放射性诊断程序。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6c66/2025464/a49f5c15eeca/brjcancer00293-0075-a.jpg

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