99mTc-CN7DG: A Highly Expected SPECT Imaging Agent of Cancer with Satisfactory Tumor Uptake and Tumor-to-Nontarget Ratios

被引：13

作者：

Gan, Qianqian ^{[1
]}

Zhang, Xuran ^{[1
]}

Ruan, Qing ^{[1
]}

Fang, Si'an ^{[1
]}

Zhang, Junbo ^{[1
]}

机构：

[1] Beijing Normal Univ, Key Lab Radiopharmaceut, Coll Chem, Minist Educ, Beijing 100875, Peoples R China

来源：

MOLECULAR PHARMACEUTICS | 2021年 / 18卷 / 03期

基金：

中国国家自然科学基金;

关键词：

Tc-99m; glucose derivatives; isocyanide ligands; imaging agents; cancer;

D O I：

10.1021/acs.molpharmaceut.0c01177

中图分类号：

R-3 [医学研究方法]; R3 [基础医学];

学科分类号：

1001 ;

摘要：

A novel glucose derivative (CN7DG) possessing an isonitrile as a coordinating group was synthesized, and Tc-99m-CN7DG, which was expected to be a powerful tumor imaging agent for SPECT, was prepared in a kit by the reaction of CN7DG with SnCl2 center dot 2H(2)O and (TcO4-)-Tc-99m. Tc-99m-CN7DG exhibited good stability and was transported via glucose transporters. Biodistribution results in mice bearing A549 tumor models showed that Tc-99m-CN7DG had a higher uptake at the tumor sites and better tumor/blood and tumor/muscle ratios than did [F-18]FDG and Tc-99m-CN5DG. SPECT/CT imaging studies showed obvious accumulation in tumor sites, suggesting that Tc-99m-CN7DG is a promising candidate for tumor imaging. Because Tc-99m and Re-188 stand for a "theranostic pair", Re-188-CN7DG is expected to be prepared as a promising agent for tumor therapy.

引用

页码：1356 / 1363

页数：8

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