Abstract

Objective: This study aimed to synthesize ¹¹C-methyl-N-2β-methylester-3β-(4-fluoropheny1) nitrilimine (¹¹C-β-CFT) using the CFN-MPS200 automated synthesis module, perform rigorous quality evaluations and subsequently conduct intracranial PET/MR imaging in patients diagnosed with Parkinson’s Disease (PD) following intravenous administration of the radiotracer.
Methods: The precursor, 2β-methyl ester-3β-(4-fluoropheny1) desmethy1nortilidine, was utilized for the synthesis of ¹¹C-β-CFT in a solvent-free environment using the Sumitomo CFN-MPS200 automated synthesis module. Comprehensive quality control measures were implemented, including radioactive high-performance liquid chromatography (Radio-HPLC), radioactive thin-layer chromatography (Radio-TLC) and endotoxin testing. Following intravenous administration of the synthesized compound, PET/MR imaging was performed on PD patients.
Results: The automated synthesis of ¹¹C-β-CFT via the CFN-MPS200 module was completed in approximately 15±2 minutes, yielding a decay-corrected production rate of (34±5)% (n=50). The radiochemical purity exceeded 90% and the radioactive concentration was approximately 850±80MBq/mL. The final product is presented as a colorless, transparent solution with a pH ranging from 7.0to8.0PET/MR imaging, conducted 40 to 50 minutes post-injection of ¹¹C-β-CFT in PD patients, demonstrated symmetrical distribution in the bilateral caudate nucleus, putamen and globus pallidus in healthy controls, whereas diminished uptake was observed in these regions among PD patients.
Conclusion: The synthesis protocol for ¹¹C-β-CFT using the CFN-MPS200 multifunctional synthesis module exhibits commendable stability and high yield, with all quality control and toxicity assessment parameters conforming to the standards set forth in the Chinese Pharmacopoeia. These findings confirm that the developed methodology can produce formulations that fulfill the requirements for both research and clinical applications, thereby establishing a foundation for future PET/MR imaging studies in PD

Keywords:Parkinson’s disease (PD); PET/MR Imaging agent; ¹¹C-β-CFT; Automated synthesis