Biological evaluation and SPECT imaging of tumor hypoxia using a novel technetium-99m labeled tracer with 2-nitroimidazole moiety
AbstractAbstract
[en] 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. (author)
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Journal of Radioanalytical and Nuclear Chemistry; ISSN 0236-5731; ; CODEN JRNCDM; v. 317(3); p. 1463-1468
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ALCOHOLS, ANTINEOPLASTIC DRUGS, AZOLES, BETA DECAY RADIOISOTOPES, BETA-MINUS DECAY RADIOISOTOPES, DISEASES, DISTRIBUTION, DRUGS, HETEROCYCLIC COMPOUNDS, HOURS LIVING RADIOISOTOPES, HYDROXY COMPOUNDS, IMIDAZOLES, INTERMEDIATE MASS NUCLEI, INTERNAL CONVERSION RADIOISOTOPES, ISOMERIC TRANSITION ISOTOPES, ISOTOPE APPLICATIONS, ISOTOPES, NITRO COMPOUNDS, NUCLEI, ODD-EVEN NUCLEI, ORGANIC COMPOUNDS, ORGANIC NITROGEN COMPOUNDS, PROCESSING, RADIOISOTOPES, RADIOSENSITIZERS, RESPONSE MODIFYING FACTORS, TECHNETIUM ISOTOPES, YEARS LIVING RADIOISOTOPES
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