机构：[1]Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, 19 Xinjiekou Outer Street, Beijing 100875, China[2]Center for Molecular Imaging and Translational Medicine, State Key Laboratory of Molecular Vaccinology and Molecular Diagnostics, School of Public Health, Xiamen University, Xiang’an South Road, Xiamen 361102, China[3]Department of Nuclear Medicine, Cardiovascular Institute and FuWai Hospital, Chinese Academy of Medical Sciences, Beijing 100037, China[4]Key Laboratory of Nuclear Radiation and Nuclear Energy Technology, Institute of High Energy Physics, Chinese Academy of Sciences, Beijing 100049, China[5]PET Center of Xuanwu Hospital, Capital Medical University, Beijing 100053, China首都医科大学宣武医院[6]College of Chemistry, Beijing Normal University, 19 Xinjiekou Outer St., Beijing 100875, China.
Lipophilic cations such as phosphonium salts can accumulate in mitochondria of heart in response to the negative inner-transmembrane potentials. Two phosphonium salts [F-18]FMBTP and [F-18]mFMBTP were prepared and evaluated as potential myocardial perfusion imaging (MPI) agents in this study. The cations were radiolabeled via a simplified one-pot method starting from [F-18]fluoride and followed by physicochemical property tests, in vitro cellular uptake assay, ex vivo mouse biodistribution, and in vivo rat microPET imaging. The total radiosynthesis time was less than 60 min including HPLC purification. The [F-18] labeled compounds were obtained in high radiolabeling yield (similar to 50%) and good radiochemical purity (>99%). Both compounds were electropositive, and their log P values at pH 7.4 were 1.16 +/- 0.003 (n = 3) and 1.05 +/- 0.01 (n = 3), respectively. Both [F-18]FMBTP and [F-18]mFMBTP had high heart uptake (25.24 +/- 2.97% ID/g and 31.02 +/- 0.33% ID/g at 5 min postinjection (p.i.)) in mice with good retention (28.99 +/- 3.54% ID/g and 26.82 +/- 3.46% ID/g at 120 min p.i.). From the PET images in rats, the cations exhibited high myocardium uptake and fast clearance from liver and small intestine to give high-contrast images across all time points. These phosphonium cations were radiosynthesized via a highly efficient one-pot procedure for potential MPI offering high heart accumulation and rapid nontarget clearance.
基金：
the National Key Basic Research Program of China (2014CB744503)
the National Natural Science Foundation of China (21271030, 20871020,81301251)
Department of Nuclear Medicine of Peking Union Medical College Hospital
语种：
外文
被引次数：
WOS：
PubmedID：
中科院(CAS)分区：
出版当年[2013]版：
大类|2 区医学
小类|2 区药学
最新[2023]版：
大类|2 区医学
小类|2 区药学3 区医学：研究与实验
JCR分区：
出版当年[2012]版：
Q1PHARMACOLOGY & PHARMACY
最新[2023]版：
Q1PHARMACOLOGY & PHARMACYQ2MEDICINE, RESEARCH & EXPERIMENTAL
第一作者机构：[1]Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, 19 Xinjiekou Outer Street, Beijing 100875, China[6]College of Chemistry, Beijing Normal University, 19 Xinjiekou Outer St., Beijing 100875, China.
通讯作者：
通讯机构：[*1]School of Public Health, Xiamen University, Xiang’an South Rd., Xiang’an district, Xiamen 361102, China
推荐引用方式(GB/T 7714)：
Zuoquan Zhao,Qian Yu,Tiantian Mou,et al.Highly Efficient One-Pot Labeling of New Phosphonium Cations with Fluorine-18 as Potential PET Agents for Myocardial Perfusion Imaging[J].MOLECULAR PHARMACEUTICS.2014,11(11):3823-3831.doi:10.1021/mp500216g.
APA：
Zuoquan Zhao,Qian Yu,Tiantian Mou,Chang Liu,Wenjiang Yang...&Xianzhong Zhang.(2014).Highly Efficient One-Pot Labeling of New Phosphonium Cations with Fluorine-18 as Potential PET Agents for Myocardial Perfusion Imaging.MOLECULAR PHARMACEUTICS,11,(11)
MLA：
Zuoquan Zhao,et al."Highly Efficient One-Pot Labeling of New Phosphonium Cations with Fluorine-18 as Potential PET Agents for Myocardial Perfusion Imaging".MOLECULAR PHARMACEUTICS 11..11(2014):3823-3831
