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• W2013374328 abstract "Two radiofluoro-pegylated phenylbenzoxazole derivatives, 4-(5-(2-(2-(2-[18F]fluoroethoxy)ethoxy)ethoxy)benzo[d]oxazol-2-yl)-N-methylaniline ([18F]24) and 4-(5-(2-(2-(2-[18F]fluoroethoxy)ethoxy)ethoxy)benzo[d]oxazol-2-yl)-N,N-dimethylaniline ([18F]32), were synthesized and evaluated as probes for imaging cerebral β-amyloid (Aβ) plaques in living brain tissue by PET. [18F]24 and [18F]32 displayed high affinity for Aβ1–42 aggregates (Ki = 9.3 and 3.9 nM, respectively). In vitro autoradiography with sections of post-mortem AD brain and transgenic mouse brain confirmed the affinity of these tracers. Initial high uptake into and rapid washout from the brain in normal mice were observed. [18F]24 also displayed excellent binding to Aβ plaques in ex vivo autoradiographic experiments with Tg2576 mice. Furthermore, small-animal PET studies demonstrated significant differences in the clearance profile after the administration of [18F]24 between Tg2576 and wild-type mice. The results suggest [18F]24 to be a useful PET agent for detecting Aβ plaques in the living human brain." @default.
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• W2013374328 date "2012-06-12" @default.
• W2013374328 modified "2023-10-01" @default.
• W2013374328 title "Novel ¹⁸F-Labeled Benzoxazole Derivatives as Potential Positron Emission Tomography Probes for Imaging of Cerebral β-Amyloid Plaques in Alzheimer’s Disease" @default.
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• W2013374328 doi "https://doi.org/10.1021/jm300251n" @default.
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