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Molecules. 2016 Dec 9;21(12). pii: E1696.

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

Author information

1
Department of Nuclear Medicine, West China Hospital of Sichuan University, Chengdu 610041, China. wenjie.zhang@yale.edu.
2
PET Center, Department of Radiology and Biomedical Imaging, Yale University, New Haven, CT 06520, USA. zhengxin.cai@yale.edu.
3
Department of Nuclear Medicine, West China Hospital of Sichuan University, Chengdu 610041, China. lilinhuaxi@sina.com.
4
PET Center, Department of Radiology and Biomedical Imaging, Yale University, New Haven, CT 06520, USA. jim.ropchan@yale.edu.
5
PET Center, Department of Radiology and Biomedical Imaging, Yale University, New Haven, CT 06520, USA. keunpoong.lim@yale.edu.
6
Department of Medicine, Yale Translational Research Imaging Center, Yale School of Medicine, New Haven, CT 06520, USA. nabil.boutagy@yale.edu.
7
PET Center, Department of Radiology and Biomedical Imaging, Yale University, New Haven, CT 06520, USA. j.wu@yale.edu.
8
Department of Medicine, Yale Translational Research Imaging Center, Yale School of Medicine, New Haven, CT 06520, USA. john.stendahl@yale.edu.
9
Department of Radiology, Washington University School of Medicine, St. Louis, MO 63110, USA. chuw@mir.wustl.edu.
10
Department of Radiology, Washington University School of Medicine, St. Louis, MO 63110, USA. groplerr@mir.wustl.edu.
11
Department of Medicine, Yale Translational Research Imaging Center, Yale School of Medicine, New Haven, CT 06520, USA. albert.sinusas@yale.edu.
12
PET Center, Department of Radiology and Biomedical Imaging, Yale University, New Haven, CT 06520, USA. chi.liu@yale.edu.
13
PET Center, Department of Radiology and Biomedical Imaging, Yale University, New Haven, CT 06520, USA. henry.huang@yale.edu.

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.

KEYWORDS:

2-[18F]fluoroethyl azide; PET; automation; in vivo imaging; reactive oxygen species; translational study

PMID:
27941676
PMCID:
PMC5505691
DOI:
10.3390/molecules21121696
[Indexed for MEDLINE]
Free PMC Article

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