title: Synthesis and Evaluation of (18)F-labeled Pyridaben Analogues for Myocardial Perfusion Imaging in Mice, Rats and Chinese mini-swine.
abstract: This study reports three novel (18)F-labeled pyridaben analogues for potential myocardial perfusion imaging (MPI). Three precursors and the corresponding nonradioactive compounds were synthesized and characterized. The radiolabeled tracers were obtained by substituting tosyl with (18)F. The total radiosynthesis time of these tracers was 70-90 min. Typical decay-corrected radiochemical yields were 47-58%, with high radiochemical purities (>98%). Tracers were evaluated as MPI agents in vitro, ex vivo and in vivo. In the mouse biodistribution study, all three radiotracers showed high initial heart uptake (34-54% ID/g at 2 min after injection) and fast liver clearance. In the microPET imaging study, [(18)F]Fmpp2 produced heart images with good quality in both mice and rats. In the whole-body PET/CT images of mini-swine, [(18)F]Fmpp2 showed excellent initial heart standardized uptake value (SUV) (7.12 at 5 min p.i.) and good retention (5.75 at 120 min p.i.). The heart/liver SUV ratios were 4.12, 5.42 and 5.99 at 30, 60 and 120 min after injection, respectively. The favorable biological properties of [(18)F]Fmpp2 suggest that it is worth further investigation as a potential MPI agent.
authors.affiliation: Center for Molecular Imaging and Translational Medicine, State Key Laboratory of Molecular Vaccinology and Molecular Diagnostics, School of Public Health, Xiamen University, Xiamen 361005, China.|Department of Nuclear Medicine, Beijing Anzhen Hospital, Capital Medical University, Beijing 100029, China.
authors.forename: Tiantian
authors.initials: T
authors.lastname: Mou
authors.affiliation: Department of Nuclear Medicine, Cardiovascular Institute and Fu Wai Hospital, Chinese Academy of Medical Sciences, Beijing 100037, China.
authors.forename: Zuoquan
authors.initials: Z
authors.lastname: Zhao
authors.affiliation: Center for Molecular Imaging and Translational Medicine, State Key Laboratory of Molecular Vaccinology and Molecular Diagnostics, School of Public Health, Xiamen University, Xiamen 361005, China.
authors.forename: Linyi
authors.initials: L
authors.lastname: You
authors.affiliation: Center for Molecular Imaging and Translational Medicine, State Key Laboratory of Molecular Vaccinology and Molecular Diagnostics, School of Public Health, Xiamen University, Xiamen 361005, China.
authors.forename: Yesen
authors.initials: Y
authors.lastname: Li
authors.affiliation: Department of Nuclear Medicine, Beijing Anzhen Hospital, Capital Medical University, Beijing 100029, China.
authors.forename: Qian
authors.initials: Q
authors.lastname: Wang
authors.affiliation: Department of Nuclear Medicine, Cardiovascular Institute and Fu Wai Hospital, Chinese Academy of Medical Sciences, Beijing 100037, China.
authors.forename: Wei
authors.initials: W
authors.lastname: Fang
authors.affiliation: Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China.
authors.forename: Jie
authors.initials: J
authors.lastname: Lu
authors.affiliation: PET Center, Xuanwu Hospital of Capital University of Medical Sciences, Beijing, 100053, China.
authors.forename: Cheng
authors.initials: C
authors.lastname: Peng
authors.affiliation: Center for Molecular Imaging and Translational Medicine, State Key Laboratory of Molecular Vaccinology and Molecular Diagnostics, School of Public Health, Xiamen University, Xiamen 361005, China.
authors.forename: Xianzhong
authors.initials: X
authors.lastname: Zhang
mesh_terms: D000818:Animals; D004355:Drug Stability; D005462:Fluorine Radioisotopes / Q000737:chemistry; D007553:Isotope Labeling; D051379:Mice; D055414:Myocardial Perfusion Imaging / Q000379:methods; D000072078:Positron Emission Tomography Computed Tomography; D011724:Pyridazines / Q000138:chemical synthesis* / Q000737:chemistry; D011854:Radiochemistry; D019275:Radiopharmaceuticals / Q000737:chemistry; D051381:Rats; D013552:Swine; D014018:Tissue Distribution
chemical_list: D005462:Fluorine Radioisotopes; D011724:Pyridazines; D019275:Radiopharmaceuticals; C428725:pyridaben; C000615276:Fluorine-18