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小说99m Tc标记的曼诺斯衍生物作为一个非常有前途的单光子发射计算机断层扫描探测器用于瘤成像

Guangxing Yin¹, Qing Ruan^1,2, Yuhao Jiang¹

¹Key Laboratory of Radiopharmaceuticals of Ministry of Education, NMPA (National Medical Products Administration) Key Laboratory for Research and Evaluation of Radiopharmaceuticals, College of Chemistry, Beijing Normal University, Beijing 100875, P. R. China.

Journal of medicinal chemistry

|July 26, 2024

概括

一种新的标记为99m技术的曼诺斯衍生物,[99mTc]Tc-CN7DM,显示出作为SPECT瘤成像剂的前景. 在临床前模型中,它表明瘤吸收率高,目标外积累率低.

科学领域:

核医学是一种核医学.
放射化学放射化学是指辐射化学.
在瘤学瘤学.

背景情况:

使用18F-2--2-脱氧-D-葡萄糖 ([18F]FDG) 的正子发射断层扫描 (PET) 是标准的临床成像方法.
单光子发射计算机断层扫描 (SPECT) 提供了更广泛的可访问性,但缺乏可比的瘤特异性成像剂.
曼诺是一种葡萄糖表皮质,通过葡萄糖载体 (GLUT) 运输到瘤细胞中.

研究的目的:

开发一种新型的SPECT瘤成像剂,具有高瘤吸收率和有利的瘤与非目标比率.
为了合成和放射性标记一个曼诺衍生物,CN7DM,用技术-99m ([99mTc]Tc-CN7DM).

主要方法:

一种曼诺衍生物 (CN7DM) 的合成及其与技术-99m.的放射性标记.
放射性标记复合物的结构确认使用类比.
在携带瘤的小鼠模型中对[99mTc]Tc-CN7DM的体内评估.

主要成果:

证实了[99mTc]Tc-CN7DM的六个协调结构.
[99mTc]Tc-CN7DM被癌细胞吸收,可能是通过GLUT和静电捕获.
在临床前研究中,该药物在非标组织中呈现出高瘤吸收率和低吸收率.

结论:

[99mTc]Tc-CN7DM显示出作为SPECT瘤成像剂的显著潜力.
开发的药物需要进一步进行癌症诊断的临床研究.

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