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
收藏
页码：39 / 45
页数：7
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