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2-(2-[2-Dimethylaminothiazol-5-yl]Ethenyl)-6- (2-[Fluoro]Ethoxy)Benzoxazole: A Novel PET Agent for In Vivo Detection of Dense Amyloid Plaques in Alzheimer's Disease Patients

¹ Tohoku University Biomedical Engineering Research Organization (TUBERO), Sendai, Japan; ² Department of Pharmacology, Tohoku University School of Medicine, Sendai, Japan; ³ Division of Cyclotron Nuclear Medicine, Cyclotron and Radioisotope Center, Tohoku University, Sendai, Japan; ⁴ Department of Geriatrics and Gerontology, Center for Asian Traditional Medicine, Tohoku University School of Medicine, Sendai, Japan; and ⁵ Division of Radiopharmaceutical Chemistry, Cyclotron and Radioisotope Center, Tohoku University, Sendai, Japan

View larger version (8K): [in this window] [in a new window]   FIGURE 1.  Chemical structures of BF-227 and BF-168 and radiosynthesis of BF-227.

View larger version (19K): [in this window] [in a new window]   FIGURE 2.  Neuropathologic staining of human brain sections by BF-227. Amyloid plaques are clearly stained with BF-227 in AD temporal brain sections (A). BF-227 staining correlates well with Aß immunostaining in adjacent sections (B, arrows). BF-227 faintly stains NFTs, in contrast to clear staining with thioflavin-S (C, arrowheads). In aged normal temporal cortex (D), no staining by BF-227 is observed. Bar in A–C = 50 µm; bar in D = 200 µm.

View larger version (33K): [in this window] [in a new window]   FIGURE 3.  In vivo binding of BF-227 to amyloid plaques in PS1/APP transgenic mouse. In brain sections from PS1/APP transgenic mouse after intravenous injection of 4 mg/kg BF-227, numerous fluorescent spots were observed in neocortex and hippocampus of brain (A and B). In contrast, no fluorescent spots were observed in brain of wild-type mouse (C). Distribution of plaques labeled with BF-227 corresponded well with Aß immunostaining in same section (B and D, arrowheads).

View larger version (20K): [in this window] [in a new window]   FIGURE 4.  Time–activity data for 11C-BF-227 PET in humans. SUV time–activity curves of 11C-BF-227 in frontal cortex (A), temporal cortex (B), parietal cortex (C), and cerebellum (D) are shown. Each point represents mean ± SEM of data from 7 AD patients and 7 normal control subjects.

View larger version (65K): [in this window] [in a new window]   FIGURE 5.  Mean SUV images between 20 and 40 min after injection of 11C-BF-227 in aged normal subject (top, 70-y-old woman) and AD patient (bottom, 68-y-old woman). Coregistered MR images are shown below PET images.

View larger version (12K): [in this window] [in a new window]   FIGURE 6.  ROI/cerebellar SUV ratio in young normal subjects (), aged normal subjects (), and AD patients (). Vertical bar represents average SUV ratio in all normal subjects (n = 11) and AD patients (n = 10).

View larger version (82K): [in this window] [in a new window]   FIGURE 7.  Brain regions show significantly elevated SUVs in AD patients compared with data from aged healthy subjects (P < 0.001, uncorrected for multiple comparisons).