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- W2017045422 abstract "6-Fluoro-PBR28 (N-(6-fluoro-4-phenoxypyridin-3-yl)-N-(2-methoxybenzyl)acetamide), a fluorinated analogue of the recently developed TSPO 18 kDa ligand PBR28, was synthesized and labelled with fluorine-18. 6-Fluoro-PBR28 and its 6-chloro/6-bromo counterparts were synthesized in six chemical steps and obtained in 16%, 10% and 19% overall yields, respectively. Labelling with fluorine-18 was performed in one single step (chlorine/bromine-for-fluorine heteroaromatic substitution) using a Zymate-XP robotic system affording HPLC-purified, ready-to-inject, 6-[18F]fluoro-PBR28 (>95% radiochemically pure). Non-decay-corrected overall yields were 9–10% and specific radioactivities ranged from 74 to 148 GBq/μmol. In vitro binding experiments, dynamic μPET studies performed in a rat model of acute neuroinflammation (unilaterally, AMPA-induced, striatum-lesioned rats) and ex vivo autoradiography on the same model demonstrated the potential of 6-[18F]fluoro-PBR28 to image the TSPO 18 kDa using PET." @default.
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- W2017045422 date "2011-08-01" @default.
- W2017045422 modified "2023-10-15" @default.
- W2017045422 title "Synthesis of 6-[18F]fluoro-PBR28, a novel radiotracer for imaging the TSPO 18kDa with PET" @default.
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- W2017045422 doi "https://doi.org/10.1016/j.bmcl.2011.06.048" @default.
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