title: Preparation and biodistribution of technetium-99m-labeled 1-(2-nitroimidazole-1-yl)-propanhydroxyiminoamide (N2IPA) as a tumor hypoxia marker.
abstract: 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.
authors.affiliation: Department of Applied Chemistry, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China.
authors.forename: Taiwei
authors.initials: T
authors.lastname: Chu
authors.forename: Rujun
authors.initials: R
authors.lastname: Li
authors.forename: Shaowen
authors.initials: S
authors.lastname: Hu
authors.forename: Xinqi
authors.initials: X
authors.lastname: Liu
authors.forename: Xiangyun
authors.initials: X
authors.lastname: Wang
mesh_terms: 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
chemical_list: D014408:Biomarkers, Tumor; D007093:Imidazoles; D015609:Organotechnetium Compounds; D019275:Radiopharmaceuticals; C493094:technetium-99m-1-(2-nitroimidazole-1-yl)-propanhydroxyiminoamide