关键词: 多发性硬化, PET显像剂, ¹¹C-CIC, 体外稳定性, 生物分布

Abstract:

Multiple sclerosis (MS) is an inflammatory neurodegenerative disorder of central nervous system. Imaging of myelin tracts in vivo would greatly improve the diagnosis and monitoring of MS. The ¹¹C-CIC was synthesized with ¹¹C-CH₃-Triflate at high yields, and was confirmed by biodistribution and imaging.  ¹¹C-CH₃-Triflate was distilled and trapped into a reaction vial containing the 2 mg precursor. The final production was purified by semi-HPLC to get ¹¹C-CIC. The in vitro stability of ¹¹C-CIC was studied at RT with or without Vc. The normal NH mice were sacrificed at different time after injection of ¹¹C-CIC for biodistribution. The micro PET/CT was performed at 30 min post-injection. The radiochemical yield was 55%65% decay corrected to ¹¹CH₃-Triflate. The radiochemical purity was over 99% at specific activity of 60 GBq/μmoL. The HPLC showed the poor stability of ¹¹C-CIC in vitro. The ¹¹C-CIC was very stable after the 10 g/L Vc used as stabilizer. The initial uptake of the cerebrum was 2.78%ID/g. The radioactivity were excreted from the digestive system and urine. The micro PET/CT imaging showed good uptake in the cerebrum. The stability of ¹¹C-CIC can be improved with Vc as stabilizer. The¹¹C-CIC was a candidate for imaging of myelin tracts for diagnosis or monitor MS.

Key words: multiple sclerosis, PET imaging agent, ¹¹C-CIC, in vitro stability, biodistribution