Preparation and biodistribution of technetium-99m-labeled 1-(2-nitroimidazole-1-yl)-propanhydroxyiminoamide (N2IPA) as a tumor hypoxia marker.
A new hydroxyiminoamide ligand, 1-(2-nitroimidazole-1-yl)-propanhydroxyiminoamide (N2IPA) was synthesized. The biodistribution of (99m)Tc-N2IPA in mice bearing S180 tumor demonstrated that the complex showed a selective accumulation in tumor and slow clearance from it. The tumor-to-tissue uptake ratios increased with time. At 4 hours after injection, the uptake ratios of tumor to muscle, blood, liver, heart, and lung reached 8.4, 1.5, 0.6, 2.9, and 2.3, respectively. Moreover, the tumor-to-liver uptake ratio steadily increased to 0.9 at 8 hours and 2.3 at 24 hours. The complex showed little uptake and quick clearance in blood, lung and other organs. Compared with other proposed hypoxia-imaging agents, this novel agent has advantages of higher tumor-to-muscle and tumor-to-blood uptake ratios and easier synthesis.
Chu
Taiwei
T
Department of Applied Chemistry, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China.
Li
Rujun
R
Hu
Shaowen
S
Liu
Xinqi
X
Wang
Xiangyun
X
D000818:Animals; D014408:Biomarkers, Tumor / Q000378:metabolism*; D015687:Cell Hypoxia; D045744:Cell Line, Tumor; D007093:Imidazoles / Q000737:chemistry / Q000493:pharmacokinetics*; D007553:Isotope Labeling / Q000379:methods; D008657:Metabolic Clearance Rate; D051379:Mice; D009928:Organ Specificity; D015609:Organotechnetium Compounds / Q000737:chemistry / Q000493:pharmacokinetics*; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000493:pharmacokinetics; D012509:Sarcoma / Q000000981:diagnostic imaging* / Q000378:metabolism*; D014018:Tissue Distribution
D014408:Biomarkers, Tumor; D007093:Imidazoles; D015609:Organotechnetium Compounds; D019275:Radiopharmaceuticals; C493094:technetium-99m-1-(2-nitroimidazole-1-yl)-propanhydroxyiminoamide