Preparation and biological evaluation of a technetium-99m labeled 4-nitroimidazole derivative for imaging tumor hypoxia

被引：8

作者：

Lin, Xiao ^{[1
,2
]}

Fang, Sian ^{[2
]}

Teng, Yanguo ^{[1
]}

Zhang, Junbo ^{[2
]}

机构：

[1] Beijing Normal Univ, Coll Water Sci, 19 Xinjiekouwai St, Beijing 100875, Peoples R China

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

来源：

JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY | 2017年 / 313卷 / 01期

基金：

中国国家自然科学基金;

关键词：

Tc-99m; 4-Nitroimidazole; Ethylene diamine tetraacetic acid; Hypoxia imaging; Tumor; MARKER; BIODISTRIBUTION; PET; METRONIDAZOLE; COMPLEXES; AGENTS;

D O I：

10.1007/s10967-017-5277-z

中图分类号：

O65 [分析化学];

学科分类号：

070302 ; 081704 ;

摘要：

A novel ethylene diamine tetraacetic acid derivative of 4-nitroimidazole (EDTA-4-EtNHNM) was successfully synthesized as a carrier molecule and it was radiolabeled with Tc-99m in high yield to obtain Tc-99m-EDTA-4-EtNHNM, which was hydrophilic and had good in vitro stability. The tumor cell experiment and the biodistribution study in mice bearing S180 tumor showed that this complex exhibited a hypoxic selectivity and had high accumulation in tumor tissue with major clearance through urinary tract. High tumor uptake and tumor/muscle ratio of the complex suggests promise towards further evaluation.

引用

页码：39 / 45

页数：7

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