title: Synthesis and radiolabeling of (64)Cu-labeled 2-nitroimidazole derivative (64)Cu-BMS2P2 for hypoxia imaging.
abstract: The objective of this study was to develop a positron emission tomography (PET) probe with hypoxia targeting specificity and a relatively long half-life. The synthesis, (64)Cu-labeling in vitro and in vivo study of the novel 2-nitroimidazole complex (64)Cu-BMS2P2 is presented in this study. The hypoxia targeting capacity of (64)Cu-BMS2P2 in vitro was evaluated and compared with the (64)Cu-BMS181321, and confirmed by PET imaging in vivo and immunohistochemistry for carbonic anhydrase 9 (CA9) in a tumor mouse model. These results suggest that (64)Cu-BMS2P2 is a promising candidate for PET hypoxia imaging and worthy of further investigations in dynamic hypoxia imaging.
authors: Key Laboratory of Carcinogenesis and Translational Research (Ministry of Education), Department of Nuclear Medicine, Peking University Cancer Hospital & Institute, Beijing 100142, PR China; PET-CT Center, The Second Xiangya Hospital of Central South University, Changsha 410011, PR China.
authors: Zheng
authors: Z
authors: Luo
authors: Key Laboratory of Carcinogenesis and Translational Research (Ministry of Education), Department of Nuclear Medicine, Peking University Cancer Hospital & Institute, Beijing 100142, PR China.
authors: Hua
authors: H
authors: Zhu
authors: Key Laboratory of Carcinogenesis and Translational Research (Ministry of Education), Department of Nuclear Medicine, Peking University Cancer Hospital & Institute, Beijing 100142, PR China.
authors: Xinfeng
authors: X
authors: Lin
authors: College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, PR China.
authors: Taiwei
authors: T
authors: Chu
authors: Department of Anesthesiology, The Second Xiangya Hospital of Central South University, Changsha 410011, PR China.
authors: Ruyi
authors: R
authors: Luo
authors: PET-CT Center, The Second Xiangya Hospital of Central South University, Changsha 410011, PR China. Electronic address: 13973186448@139.com.
authors: Yunhua
authors: Y
authors: Wang
authors: Key Laboratory of Carcinogenesis and Translational Research (Ministry of Education), Department of Nuclear Medicine, Peking University Cancer Hospital & Institute, Beijing 100142, PR China. Electronic address: pekyz@163.com.
authors: Zhi
authors: Z
authors: Yang
mesh_terms: D000818:Animals; D015687:Cell Hypoxia; D056831:Coordination Complexes / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics*; D003301:Copper Radioisotopes; D007553:Isotope Labeling; D008175:Lung Neoplasms / Q000000981:diagnostic imaging* / Q000473:pathology*; D051379:Mice; D057054:Molecular Imaging; D015394:Molecular Structure; D009374:Neoplasms, Experimental / Q000000981:diagnostic imaging / Q000473:pathology; D009593:Nitroimidazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics*; D049268:Positron-Emission Tomography; D019275:Radiopharmaceuticals / Q000032:analysis / Q000138:chemical synthesis* / Q000737:chemistry
chemical_list: C000611229:64Cu-BMS2P2; D056831:Coordination Complexes; D003301:Copper Radioisotopes; D009593:Nitroimidazoles; D019275:Radiopharmaceuticals
keywords: 2-Nitroimidazole; Carbonic anhydrase 9; Copper-64; Hypoxia imaging; Positron emission tomography