Automatic Synthesis of Myocardial Perfusion Imaging Agent ¹⁸F-BMS747158-02 and Imaging of Myocardial Ischemia Model

¹⁸F-BMS747158-02 is a fluorine-18-labeled pyridaben derivative and a new positron radionuclide myocardial perfusion imaging tracer targeting mitochondrial complex-Ⅰ. In this study, ¹⁸F-BMS747158-02 was synthesized fully automatically and applied in the imaging of acute myocardial ischemia model animals. Its imaging performance was compared with ¹³N-NH₃·H₂O, a commonly used myocardial perfusion imaging agent in China. The synthesis of ¹⁸F-BMS747158-02 was completed by three steps: nucleophilic substitution, high-performance liquid phase separation and solid phase extraction. The total synthesis time was about 60 min. The synthesis yield was (15.3±2.1)% (EOB, n=5). The radiochemical purity was greater than 99%. Imaging studies found that the ¹⁸F-BMS747158-02 myocardium had a high primary myocardial uptake rate, fast myocardial uptake, good correlation with blood perfusion, long myocardial retention time, uniform radioactive uptake, low intrahepatic uptake, and high image contrast, which confirmed the unique potential of the agent in myocardial perfusion PET imaging.