99mTc-ADP:一种潜在的体内肿瘤检测试剂。

E T León, A M Rey, E O Savio, J J López, E Kremer, A S León
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摘要

不同的研究小组提出了使用99mtc标记的核苷酸作为肿瘤寻找剂的可能性。我们最近报道了一种99mTc-ADP复合物的制备,其放射化学纯度高(> 95%),体外和体内稳定性好,并且在小鼠自发性乳腺腺癌中注射后具有良好的生物分布结果。在这里,我们报告了自发肿瘤过程动物的进一步研究结果,包括小鼠全身放射自显影(注射后20分钟和60分钟)和Wistar大鼠的γ -相机成像研究。获得动态研究(长达45分钟)和静态图像(长达18小时)以确定99mTc-ADP的药代动力学以及肿瘤/肌肉和肿瘤/血液比率。血池研究也作为对照进行。正如生物分布研究所期望的那样,肿瘤通过放射自显影显示。动态研究表明,血液清除速度快,其行为符合三颞叶模型。放射性物质被肾脏迅速吸收,并随尿液排出体外。没有证据表明该复合物在体内不稳定。注射后20分钟肿瘤摄取达到最大值。随着时间的推移,肿瘤/血液和肿瘤/肌肉的比例有所改善,增强了肿瘤的可视化。注射后3小时获得最佳图像。综上所述,我们的研究表明99mTc-ADP是一种很有前景的肿瘤诊断放射性药物。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
99mTc-ADP: a potential agent for in vivo tumor detection.

The possibility of using 99mTc-labelled nucleotides as tumour seeking agents has been proposed by different research groups. We have recently reported the preparation of a 99mTc-ADP complex with a high radiochemical purity (> 95%), good in vitro and in vivo stability and promising biodistribution results when injected in mice bearing spontaneous mammary adenocarcinomas. Here we report the results of further investigations in animals with spontaneous neoplastic processes, including whole-body autoradiography in mice (20 minutes and 60 minutes post injection) and gamma-camera imaging studies in Wistar rats. Dynamic studies (up to 45 minutes) and static images (up to 18 hours) were acquired to determine the pharmacokinetics of 99mTc-ADP and the tumour/muscle and tumour/blood ratios. Blood-pool studies were also performed as a control. Tumours were visualized by autoradiography as was to be expected from the biodistribution studies. Dynamic studies showed a rapid blood clearance and a behaviour that fitted to a tricompartimental model. Radioactivity was rapidly taken up by the kidneys and excreted in the urine. No evidence of in vivo instability of the complex was observed. Tumour uptake reached the maximum values after 20 minutes post-injection. Tumour/blood and tumour/muscle ratios improved over time, enhancing tumour visualization. The best images were obtained after 3 hours post injection. In summary, our studies suggest that 99mTc-ADP is a promising radiopharmaceutical for tumour diagnosis.

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