Biological characters of [18F]O-FEt-PIB in a rat model of Alzheimer's disease using micro-PET imaging

Ming Qiang Zheng, Duan Zhi Yin, Lan Zhang, Bei Lei, Deng Feng Cheng, Han Cheng Cai, Yan Jiang Han, Ming Xing Wu, Hong Zhang, Jing Wang

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Abstract

Aim: To evaluate whether the newly-synthesized positron emission tomography (PET) tracer, [18F]2-(4′-(methylamino)phenyl)-6-fluoroethoxy- benzothiazole ([18F] O-FEt-PIB), could bind to β-amyloid aggregates in a rat model of Alzheimer's disease (AD) using micro-PET. Method: [18F]O-FEt-PIB was synthesized and purified by radio HPLC. PET imaging was performed with a R4 rodent model scanner in 3 model and 3 control rats. Dynamic PET scans were performed for 40 min in each rat following an injection of approximately 37 MBq of [18F]O-FEt-PIB. Static scans were also performed for 15 min in each rat. PET data were reconstructed by a maximum posteriori probability algorithm. On the coronal PET images, regions of interest were respectively placed on the cortex, hemicerebrum [including the hippocampus and thalamus (HT)], and were guided by a 3-D digital map of the rat brain or the brain images of [18F]2-Deoxy-2-fluoro-JD-glucose ([ 18F]FDG) in normal rats. Time-activity curves (TAC) were obtained for the cerebrum and cerebellum. The activity difference value (ADV) between 2 hemicerebrums was also calculated. Results: The TAC for [18F]O-FEt- PIB in the cerebrum or cerebellum peaked early (at approximately 2 min), but washed out a little slowly. In the dynamic and static micro-PET images, increased radioactivity was found in the area of the right HT in the model rats where infused with β-amyloid (1-40). No distinct difference of radioactivity was found between the right and left HT areas in the control rats. The ADV(HT) was approximately 14.6% in the AD model rats and approximately 4 times greater than that of the control rats (3.9%). Conclusion: To our knowledge, this study is the first to evaluate a small molecular PET probe for the p-amyloid deposits in vivo using micro-PET imaging in an AD-injected rat model. The suitable biological characters showed that the tracer had potential to be developed as a probe for detecting β-amyloid plaques in AD.

Original languageEnglish (US)
Pages (from-to)548-554
Number of pages7
JournalActa Pharmacologica Sinica
Volume29
Issue number5
DOIs
Publication statusPublished - May 2008

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Keywords

  • [F]O-FEt-PIB
  • Alzheimer's disease
  • Micro-positron emission tomography

ASJC Scopus subject areas

  • Chemistry(all)
  • Pharmacology
  • Pharmacology (medical)

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