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Molecules 2016, 21(8), 1019;

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

PET Center, Huashan Hospital, Fudan University, Shanghai 200235, China
Department of Pathology, Shanghai Medical College, Fudan University, Shanghai 200030, China
No.6 Shanghai People’s Hospital, Jiaotong University, Shanghai 200235, China
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)
Full-Text   |   PDF [2589 KB, uploaded 5 August 2016]   |  


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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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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