Synthesis and biodistribution of a novel 99mTc-DMSA-metronidazole ester as a potential tumor hypoxia imaging agent

被引：40

作者：

Zhang, Junbo ^{[1
,2
]}

Yu, Qian ^{[1
,2
,3
]}

Huo, Jinfeng ^{[1
,2
]}

Pang, Yan ^{[1
,2
]}

Yang, Sheng ^{[1
,2
]}

He, Yining ^{[1
,2
]}

Tang, Tingting ^{[1
,2
]}

Yang, Chenchen ^{[1
,2
]}

Wang, Xuebin ^{[1
,2
]}

机构：

[1] Minist Educ, Key Lab Radiopharmaceut, Beijing 100875, Peoples R China

[2] Beijing Normal Univ, Coll Chem, Beijing 100875, Peoples R China

[3] Qingdao Univ, Affilated Hosp, Coll Med, Qingdao 266071, Peoples R China

来源：

JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY | 2010年 / 283卷 / 02期

基金：

中国国家自然科学基金;

关键词：

Dimercaptosuccinic acid; Metronidazoleester; Tc-99m; Hypoxia; Tumor; BIOLOGICAL EVALUATION; METRONIDAZOLE; COMPLEX; ACID;

D O I：

10.1007/s10967-010-0455-2

中图分类号：

O65 [分析化学];

学科分类号：

070302 ; 081704 ;

摘要：

The dimercaptosuccinic acid metronidazole ester (DMSAMe) was synthesized and radiolabeled with Tc-99m to form the Tc-99m-DMSAMe complex in high yield. The radiochemical purity of the Tc-99m-DMSAMe complex was over 90%, as measured by TLC and by HPLC, without any notable decomposition at room temperature over a period of 6 h. Its partition coefficient indicated that it was a lipophilic complex. The tumor cell experiment and the biodistribution in mice bearing S 180 tumor showed that the Tc-99m-DMSAMe complex had a certain hypoxic selectivity and accumulated in the tumor with high uptake and good retention. The tumor/blood and tumor/muscle ratios increased with time, suggesting it would be a possible tumor hypoxia imaging agent.

引用

页码：481 / 485

页数：5

共 10 条

[1]

BLOWER PJ, 1991, J NUCL MED, V32, P845

[2] PRODRUGS AS DRUG DELIVERY SYSTEMS .26. PREPARATION AND ENZYMATIC-HYDROLYSIS OF VARIOUS WATER-SOLUBLE AMINO-ACID ESTERS OF METRONIDAZOLE [J].