Optimization of Automated Radiosynthesis of 18FAV-45: A New PET Imaging Agent for Alzheimer’s Disease

摘要

IntroductionAccumulation of β-amyloid (Aβ) aggregates in the brain is linked to the pathogenesis of Alzheimer’s disease (AD). Imaging probes targeting these Aβ aggregates in the brain may provide a useful tool to facilitate the diagnosis of AD. Recently, [¹⁸F]AV-45 ([¹⁸F]>5) demonstrated high binding to the Aβ aggregates in AD patients. To improve the availability of this agent for widespread clinical application, a rapid, fully automated high yield, cGMP-compliant radiosynthesis was necessary for production of this probe. We report herein an optimal [¹⁸F]fluorination, de-protection condition and fully automated radiosynthsis of [¹⁸F]AV-45 >([¹⁸F]>5) on a radiosynthesis module (BNU F-A2).