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Molecules 2016, 21(12), 1696; doi:10.3390/molecules21121696

Optimized and Automated Radiosynthesis of [18F]DHMT for Translational Imaging of Reactive Oxygen Species with Positron Emission Tomography

1
Department of Nuclear Medicine, West China Hospital of Sichuan University, Chengdu 610041, China
2
PET Center, Department of Radiology and Biomedical Imaging, Yale University, New Haven, CT 06520, USA
3
Department of Medicine, Yale Translational Research Imaging Center, Yale School of Medicine, New Haven, CT 06520, USA
4
Department of Radiology, Washington University School of Medicine, St. Louis, MO 63110, USA
*
Authors to whom correspondence should be addressed.
Academic Editor: Zhen Cheng
Received: 18 October 2016 / Revised: 27 November 2016 / Accepted: 2 December 2016 / Published: 9 December 2016
(This article belongs to the Special Issue Molecular Imaging Probes)
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Abstract

Reactive oxygen species (ROS) play important roles in cell signaling and homeostasis. However, an abnormally high level of ROS is toxic, and is implicated in a number of diseases. Positron emission tomography (PET) imaging of ROS can assist in the detection of these diseases. For the purpose of clinical translation of [18F]6-(4-((1-(2-fluoroethyl)-1H-1,2,3-triazol-4-yl)methoxy)phenyl)-5-methyl-5,6-dihydrophenanthridine-3,8-diamine ([18F]DHMT), a promising ROS PET radiotracer, we first manually optimized the large-scale radiosynthesis conditions and then implemented them in an automated synthesis module. Our manual synthesis procedure afforded [18F]DHMT in 120 min with overall radiochemical yield (RCY) of 31.6% ± 9.3% (n = 2, decay-uncorrected) and specific activity of 426 ± 272 GBq/µmol (n = 2). Fully automated radiosynthesis of [18F]DHMT was achieved within 77 min with overall isolated RCY of 6.9% ± 2.8% (n = 7, decay-uncorrected) and specific activity of 155 ± 153 GBq/µmol (n = 7) at the end of synthesis. This study is the first demonstration of producing 2-[18F]fluoroethyl azide by an automated module, which can be used for a variety of PET tracers through click chemistry. It is also the first time that [18F]DHMT was successfully tested for PET imaging in a healthy beagle dog. View Full-Text
Keywords: PET; reactive oxygen species; in vivo imaging; automation; 2-[18F]fluoroethyl azide; translational study PET; reactive oxygen species; in vivo imaging; automation; 2-[18F]fluoroethyl azide; translational study
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Zhang, W.; Cai, Z.; Li, L.; Ropchan, J.; Lim, K.; Boutagy, N.E.; Wu, J.; Stendahl, J.C.; Chu, W.; Gropler, R.; Sinusas, A.J.; Liu, C.; Huang, Y. Optimized and Automated Radiosynthesis of [18F]DHMT for Translational Imaging of Reactive Oxygen Species with Positron Emission Tomography. Molecules 2016, 21, 1696.

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