Optimization and biodistribution of [11C]-TKF, an analog of tau protein imaging agent [18F]-THK523

Yanyan Kong, Yihui Guan, Fengchun Hua, Zhengwei Zhang, Xiuhong Lu, Tengfang Zhu, Bizeng Zhao, Jianhua Zhu, Cong Li, Jian Chen

Research output: Contribution to journalArticle

Abstract

The quantification of neurofibrillary tangles (NFTs) using specific PET tracers can facilitate the diagnosis of Alzheimer's disease (AD) and allow monitoring of disease progression and treatment efficacy. [18F]-THK523 has shown high affinity and selectivity for tau pathology. However, its high retention in white matter, which makes simple visual inspection difficult, may limit its use in research or clinical settings. In this paper, we optimized the automated radiosynthesis of [11C]-TKF and evaluated its biodistribution and toxicity in C57 mice. [11C]-TKF can be made by reaction precursor with [11C]MeOTf or 11CH3I, but [11C]MeOTf will give us higher labeling yields and specific activity. [11C]-TKF presented better brain uptake in normal mouse than [18F]-THK523 (3.23% ± 1.25% ID·g-1 vs. 2.62% ± 0.39%ID·g-1 at 2 min post-injection). The acute toxicity studies of [11C]-TKF were unremarkable.

Original languageEnglish (US)
Article number1019
JournalMolecules
Volume21
Issue number8
DOIs
Publication statusPublished - Aug 1 2016
Externally publishedYes

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Keywords

  • Alzheimer's disease
  • Imaging
  • Neurofibrillary tangles (NFTs)
  • Positron emission tomography (PET)
  • Tau

ASJC Scopus subject areas

  • Organic Chemistry

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