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- Title
Biological evaluation and SPECT imaging of tumor hypoxia using a novel technetium-99m labeled tracer with 2-nitroimidazole moiety.
- Authors
Lin, Xiao; Ruan, Qing; Lin, Ling; Zhang, Xuran; Duan, Xiaojiang; Teng, Yanguo; Zhang, Junbo
- Abstract
To develop novel 99mTc labeled nitroimidazole imaging agents for imaging tumor hypoxia, 99mTc labeled ethylene diamine tetraacetic acid derivative of 4-nitroimidazole was reported by us earlier, which showed disadvantage of an unsatisfactory tumor-to-blood ratio. Therefore, 2-nitroimidazole was adopted as a pharmacophore to synthesize EDTA-2-EtNHNM, which was radiolabeled with 99mTc in high yield to achieve 99mTc-EDTA-2-EtNHNM. 99mTc-EDTA-2-EtNHNM was hydrophilic and exhibited good in vitro stability. Cellular experiment demonstrated its hypoxic selectivity while biodistribution results showed improved tumor-to-blood and tumor-to-muscle ratios. SPECT imaging studies of 99mTc-EDTA-2-EtNHNM indicated obvious accumulation in tumor, suggesting its potential to be a radiotracer for imaging tumor hypoxia.
- Subjects
HYPOXEMIA; NITROIMIDAZOLES; IMIDAZOLES; NITRO compounds; RADIATION-sensitizing agents
- Publication
Journal of Radioanalytical & Nuclear Chemistry, 2018, Vol 317, Issue 3, p1463
- ISSN
0236-5731
- Publication type
Article
- DOI
10.1007/s10967-018-6005-z