机构：[1]Department of Nuclear Medicine, Beijing Anzhen Hospital, Capital Medical University, Beijing 100029, China[2]Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China[3]Center for Molecular Imaging and Translational Medicine, State Key Laboratory of Molecular Vaccinology and Molecular Diagnostics, School of Public Health, Xiamen University, Xiamen 361102, China[4]Department of Nuclear Medicine, Cardiovascular Institute and Fuwai Hospital, Chinese Academy of Medical Sciences, Beijing 100037, China[5]Beijing PET Center of Xuanwu Hospital, Capital Medical University, Beijing 100053, China首都医科大学宣武医院
To improve the stability of F-18-labeled pyridaben analogs for myocardial perfusion imaging, three new analogs of pyridaben ([F-18]FPTP2, [F-18]FPTP-P2, and [F-18]FPTP-P3) were synthesized with side chain' modifications. The radiolabeled tracers and corresponding non-radioactive compounds were obtained by substituting tosyl group with F-18/19. The effect of structure modification on myocardial targeting and physicochemical properties of new tracers were evaluated in vitro and in vivo. The total radiosynthesis time of these tracers was approximately 70-90min with high decay-corrected radiochemical yields (36-65%) and good radiochemical purity (>98%). These lipophilic tracers exhibited obvious improved stability in water. Studies of their biodistribution in normal Kunming mice demonstrated that [F-18]FPTP2 exhibited very high initial heart uptake (39.70 +/- 2.81%ID/g at 2min after injection) and low background in the liver, blood, and soft tissues. The heart-to-liver, heart-to-lung, and heart-to-blood ratios were 3.59, 19.34, and 67.34 at 15min postinjection, respectively. Favorable myocardial targeting property and remarkable improvement of stability of [F-18]FPTP2 suggest that the substitution of the phenyl sidechain' with other non-phenyl rings hasno effect on the myocardial targeting property of F-18-labeled pyridaben analogs.
基金：
the National Key Basic Research Program of China (2014CB744503)
National Natural Science Foundation of China (81471707, 21271030, 81301251, 81271613),
the Fundamental Research Funds for the Central Universities of China (2013SH009).
第一作者机构：[1]Department of Nuclear Medicine, Beijing Anzhen Hospital, Capital Medical University, Beijing 100029, China[2]Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China
共同第一作者：
通讯作者：
通讯机构：[3]Center for Molecular Imaging and Translational Medicine, State Key Laboratory of Molecular Vaccinology and Molecular Diagnostics, School of Public Health, Xiamen University, Xiamen 361102, China
推荐引用方式(GB/T 7714)：
Tiantian Mou,Zuoquan Zhao,Pu Zhang,et al.Synthesis and Bio-Evaluation of New F-18-Labeled Pyridaben Analogs with Improved Stability for Myocardial Perfusion Imaging in Mice[J].CHEMICAL BIOLOGY & DRUG DESIGN.2015,86(3):351-361.doi:10.1111/cbdd.12499.
APA：
Tiantian Mou,Zuoquan Zhao,Pu Zhang,Wei Fang,Cheng Peng...&Xianzhong Zhang.(2015).Synthesis and Bio-Evaluation of New F-18-Labeled Pyridaben Analogs with Improved Stability for Myocardial Perfusion Imaging in Mice.CHEMICAL BIOLOGY & DRUG DESIGN,86,(3)
MLA：
Tiantian Mou,et al."Synthesis and Bio-Evaluation of New F-18-Labeled Pyridaben Analogs with Improved Stability for Myocardial Perfusion Imaging in Mice".CHEMICAL BIOLOGY & DRUG DESIGN 86..3(2015):351-361
