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

Junbo Zhang; Qian Yu; Jinfeng Huo; Yan Pang; Sheng Yang; Yining He; Tingting Tang; Chenchen Yang; Xuebin Wang

doi:10.1007/s10967-010-0455-2

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Journal of Radioanalytical and Nuclear Chemistry

Volume/Issue:: Volume 283: Issue 2

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

Authors:

Junbo Zhang

Junbo Zhang

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Qian Yu

Qian Yu

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Jinfeng Huo

Jinfeng Huo

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Yan Pang

Yan Pang

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Sheng Yang

Sheng Yang

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Yining He

Yining He

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Tingting Tang

Tingting Tang

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Chenchen Yang

Chenchen Yang

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Xuebin Wang

Xuebin Wang

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Pages:: 481–485

Online Publication Date:: 27 Jan 2010

Publication Date:: 01 Feb 2010

Article Category:: Research Article

DOI:: https://doi.org/10.1007/s10967-010-0455-2

Keywords:: Dimercaptosuccinic acid; Metronidazole ester; 99mTc; Hypoxia; Tumor

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Abstract

The dimercaptosuccinic acid metronidazole ester (DMSAMe) was synthesized and radiolabeled with ^99mTc to form the ^99mTc-DMSAMe complex in high yield. The radiochemical purity of the ^99mTc-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 ^99mTc-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.

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Journal of Radioanalytical and Nuclear Chemistry

Print ISSN:: 0236-5731

Online ISSN:: 1588-2780

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Journal of Radionalytical and Nuclear Chemistry
Language	English
Size	A4
Year of Foundation	1968
Volumes per Year	1
Issues per Year	12
Founder	Akadémiai Kiadó
Founder's Address	H-1117 Budapest, Hungary 1516 Budapest, PO Box 245.
Publisher	Akadémiai Kiadó Springer Nature Switzerland AG
Publisher's Address	H-1117 Budapest, Hungary 1516 Budapest, PO Box 245. CH-6330 Cham, Switzerland Gewerbestrasse 11.
Responsible Publisher	Chief Executive Officer, Akadémiai Kiadó
ISSN	0236-5731 (Print)
ISSN	1588-2780 (Online)