Journal of Radioanalytical and Nuclear Chemistry
Volume/Issue:
Volume 287: Issue 3
Synthesis and biodistribution of a novel 99mTc complex of HYNIC-conjugated metronidazole as a potential tumor hypoxia imaging agent
Authors:
Liqin Liu Department of Biological Science and Engineering, School of Chemical and Biological Engineering, University of Science and Technology Beijing, 30th Xueyuan Road, Haidian District, Beijing, 100083 People’s Republic of China

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Min Zhang Department of Biological Science and Engineering, School of Chemical and Biological Engineering, University of Science and Technology Beijing, 30th Xueyuan Road, Haidian District, Beijing, 100083 People’s Republic of China

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Guangrong Zhong Department of Biological Science and Engineering, School of Chemical and Biological Engineering, University of Science and Technology Beijing, 30th Xueyuan Road, Haidian District, Beijing, 100083 People’s Republic of China

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Xuebin Wang Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education, College of Chemistry, Beijing Normal University, Beijing, 100875 People’s Republic of China

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Pages:
847–852
Online Publication Date:
01 Nov 2010
Publication Date:
01 Mar 2011
Article Category:
Research Article
DOI:
https://doi.org/10.1007/s10967-010-0889-6
Keywords:
99mTc; HYNIC; Bifunctional chelator; Hypoxia imaging agent; Metronidazole
Restricted access

Abstract  

A conjugate of 6-hydrazinopyridine-3-carboxylic acid (HYNIC) with the amino analogue of metronidazole (MN) was synthesized through a multiple-step reaction. HYNIC-MN could be labeled easily and efficiently with 99mTc using N-(2-hydroxy-1,1-bis(hydroxymethyl)ethyl)glycine (tricine) and ethylenediamine -N,N′-diacetic acid (EDDA) as coligands to form the 99mTc–HYNIC–MN complex in high yield (>95%). Its partition coefficient indicated that it was a good hydrophilic complex. The tumor cell experiment showed that the 99mTc–HYNIC–MN complex had a certain hypoxic selectivity. The biodistribution studies of 99mTc–HYNIC–MN in Kunming mice bearing S180 tumor showed a favorable tissue distribution profile with high tumor uptake, and low or negligible accumulation in non-target organs, suggesting 99mTc–HYNIC–MN would be a novel potential tumor hypoxia imaging agent.

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Cover Journal of Radioanalytical and Nuclear Chemistry
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)

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