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- Title
Optimized and Automated Radiosynthesis of [<sup>18</sup>F]DHMT for Translational Imaging of Reactive Oxygen Species with Positron Emission Tomography.
- Authors
Wenjie Zhang; Zhengxin Cai; Lin Li; Ropchan, Jim; Keunpoong Lim; Boutagy, Nabil E.; Jing Wu; Stendahl, John C.; Wenhua Chu; Gropler, Robert; Sinusas, Albert J.; Chi Liu; Yiyun Huang
- 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.
- Subjects
REACTIVE oxygen species; POSITRON emission tomography; CELL communication; HOMEOSTASIS; RADIOCHEMICAL yield
- Publication
Molecules, 2016, Vol 21, Issue 12, p1696
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules21121696