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• W67111611 abstract "623 Objectives: It is well known that accumulation of beta-amyloid (Abeta) plaques in the brain is implicated in the development of Alzheimer’s disease (AD). PET imaging studies in humans have been performed using the amyloid binding 11C radiotracer Pittsburgh Compound B (PIB). The results suggest that this imaging agent may be useful for diagnosis of AD. To improve the potential of this imaging technique for routine clinical studies, we have developed a novel series of 18F labeled fluoro-polyethylene glycol (FPEG) derivatives of PIB as PET imaging agents targeting Abeta plaques in the brain. We are particularly interested to investigate the size of FPEG and its effects on in vitro binding affinity as well as in vivo biodistribution (brain penetration in normal mice). Methods: The FPEG-PIB derivatives used in the study were synthesized starting from 2-(aminophenyl)-6-hydroxy-benzothiozole, which on N-monomethylation afforded the PIB compound. Subsequent alkylation of the hydroxyl group of PIB with various FPEG chloride or bromide gave the corresponding FPEG-PIB derivatives in 70-80% yield. Binding studies were evaluated using postmortem AD brain homogenates and biodistribution studies were carried out in normal mice. The F-18 compounds were prepared by K[F-18]F/K[2,2,2] displacement of MsO-derivative in exceelent yields. Results: In vitro competitive binding studies of compounds with [125I]-IMPY established that adding various length of FPEG group (n = 2-8) has little impact on the binding affinities (Ki = 2-9 nM). In vivo biodistribution studies of 18F labeled FPEG-PIB derivatives in normal mice showed initial brain uptake in the brain was 5.53 and 2.57 %dose/g at 2 min for n = 3 and 6, respectively; while the partition coefficient showed a comparable value (logP = 3.04 and 2.99, respectively). In vitro autoradiography using postmortem brain tissue sections suggested that n = 3 derivative has a more distinctive labeling of the plaques than that of n = 6 derivative. Conclusions: The preliminary studies established the structure activity relationship (SAR) of PIB derivatives and the initial data clearly show that FPEG-PIB n = 3 derivative is a suitable candidates for the development of novel Abeta plaque imaging agents. Research Support (if any): NIH AG-22559" @default.
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• W67111611 date "2006-05-01" @default.
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• W67111611 title "2-Arylbenzothiazole derivatives for beta-amyloid plaque imaging" @default.
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