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Molecules 2016, 21(8), 1019; doi:10.3390/molecules21081019

Optimization and Biodistribution of [11C]-TKF, An Analog of Tau Protein Imaging Agent [18F]-THK523

1
PET Center, Huashan Hospital, Fudan University, Shanghai 200235, China
2
Department of Pathology, Shanghai Medical College, Fudan University, Shanghai 200030, China
3
No.6 Shanghai People’s Hospital, Jiaotong University, Shanghai 200235, China
4
Key Laboratory of Smart Drug Delivery, Ministry of Education & PLA, School of Pharmacy, Fudan University, Shanghai 201203, China
*
Author to whom correspondence should be addressed.
Academic Editors: Michael Decker and Diego Muñoz-Torrero
Received: 27 May 2016 / Revised: 1 August 2016 / Accepted: 3 August 2016 / Published: 5 August 2016
(This article belongs to the Special Issue Molecules against Alzheimer)
View Full-Text   |   Download PDF [2589 KB, uploaded 5 August 2016]   |  

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. View Full-Text
Keywords: Alzheimer’s disease; positron emission tomography (PET); tau; neurofibrillary tangles (NFTs); imaging Alzheimer’s disease; positron emission tomography (PET); tau; neurofibrillary tangles (NFTs); imaging
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Kong, Y.; Guan, Y.; Hua, F.; Zhang, Z.; Lu, X.; Zhu, T.; Zhao, B.; Zhu, J.; Li, C.; Chen, J. Optimization and Biodistribution of [11C]-TKF, An Analog of Tau Protein Imaging Agent [18F]-THK523. Molecules 2016, 21, 1019.

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