Authors:
Jianjun Wang Radiochemistry Lab, School of Nuclear Science and Technology, Lanzhou University, Lanzhou, 730000 People’s Republic of China

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Yuan Tian Radiochemistry Lab, School of Nuclear Science and Technology, Lanzhou University, Lanzhou, 730000 People’s Republic of China

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Xiaojiang Duan Radiochemistry Lab, School of Nuclear Science and Technology, Lanzhou University, Lanzhou, 730000 People’s Republic of China

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Jing Yang Radiochemistry Lab, School of Nuclear Science and Technology, Lanzhou University, Lanzhou, 730000 People’s Republic of China

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Huining Mao Radiochemistry Lab, School of Nuclear Science and Technology, Lanzhou University, Lanzhou, 730000 People’s Republic of China

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Cunmin Tan Radiochemistry Lab, School of Nuclear Science and Technology, Lanzhou University, Lanzhou, 730000 People’s Republic of China

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Wangsuo Wu Radiochemistry Lab, School of Nuclear Science and Technology, Lanzhou University, Lanzhou, 730000 People’s Republic of China

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Abstract  

This study reports the synthesis, radiolabeling and preliminary biodistribution results of [99mTc(CO)3(MN-TZ-BPA)]+ in tumor-bearing mice. The novel nitroimidazole derivative was successfully synthesized by conjugation of bis(pyridin-2-ylmethyl)amine (BPA) to 2-methyl-5-niroimidazole via “click” reaction. The ligand could be labeled by [99mTc(CO)3]+ core in high yield to get [99mTc(CO)3(MN-TZ-BPA)]+, which was very hydrophilic and was stable at room temperature. Biodistribution studies in tumor-bearing mice showed that [99mTc(CO)3(MN-TZ-BPA)]+ accumulated in the tumor with certain initial uptake while poor retention. The rapid clearance from normal organs with favorable tumor/muscle ratios warrants further research to improve tumor targeting efficacy and pharmacokinetic profile of radiolabeled nitroimidazoles by structural modification.

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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)