Abstract | INTRODUCTION: METHODS: Nine nitroimidazole (2-, 4- and 5-nitroimidazole) ligands were synthesized and radiolabeled using [(99m)Tc(CO)3(H2O)3](+) precursor to obtain a group of complexes possessing different single electron reduction potential (SERP), overall charge and lipophilicity, the three attributes which decide the efficacy of the complex to detect hypoxic cells in vivo. The nitroimidazole-(99m)Tc(CO)3 complexes as well as [(18)F] FMISO were evaluated in fibrosarcoma tumor bearing mice. RESULTS: CONCLUSIONS: Results of the present study indicated that uptake of the radiotracer in tumor is closely associated with its rate of clearance from blood. The study also indicated that along with SERP, clearance of radiotracer from blood (net effect of charge and lipophilicity) is a critical factor which decides the in vivo efficacy of the hypoxia detecting radiopharmaceutical.
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Authors | Madhava B Mallia, Suresh Subramanian, Anupam Mathur, H D Sarma, Sharmila Banerjee |
Journal | Nuclear medicine and biology
(Nucl Med Biol)
Vol. 41
Issue 7
Pg. 600-10
(Aug 2014)
ISSN: 1872-9614 [Electronic] United States |
PMID | 24856280
(Publication Type: Journal Article)
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Copyright | Copyright © 2014 Elsevier Inc. All rights reserved. |
Chemical References |
- Biomarkers, Tumor
- Nitroimidazoles
- Organotechnetium Compounds
- 4-nitroimidazole
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Topics |
- Animals
- Biological Transport
- Biomarkers, Tumor
(chemistry, metabolism, pharmacokinetics)
- Cell Hypoxia
- Fibrosarcoma
(pathology)
- Humans
- Hydrophobic and Hydrophilic Interactions
- Mice
- Nitroimidazoles
(chemistry)
- Organotechnetium Compounds
(chemistry, metabolism, pharmacokinetics)
- Radiochemistry
- Tissue Distribution
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