On December 2, 2019, Chen, Junyi; Li, Cong; Hong, Hanyu; Liu, Hui; Wang, Chunhong; Xu, Mengxin; Han, Yuxiang; Liu, Zhibo published an article.Reference of Methyl 6-chloro-6-oxohexanoate The title of the article was Side Chain Optimization Remarkably Enhances the in Vivo Stability of 18F-Labeled Glutamine for Tumor Imaging. And the article contained the following:
Similar to glycolysis, glutaminolysis acts as a vital energy source in tumor cells, providing building blocks for the metabolic needs of tumor cells. To capture glutaminolysis in tumors, 18F-(2S,4R)4-fluoroglutamine ([18F]FGln) and 18F-fluoroboronoglutamine ([18F]FBQ) have been successfully developed for positron emission tomog. (PET) imaging, but these two mols. lack stability, resulting in undesired yet significant bone uptake. In this study, we found that [18F]FBQ-C2 is a stable Gln PET tracer by adding two more methylene groups to the side chain of [18F]FBQ. [18F]FBQ-C2 was synthesized with a good radiochem. yield of 35% and over 98% radiochem. purity. [18F]FBQ-C2 showed extreme stability in vitro, and no defluorination was observed after 2 h in phosphate buffered saline at 37°C. The competitive inhibition assay results indicated that [18F]FBQ-C2 enters cells via the system ASC and N, similar to natural glutamine, and can be transported by tumor-overexpressed ASCT2. PET imaging and biodistribution results indicated that [18F]FBQ-C2 is stable in vivo with low bone uptake (0.81 ± 0.20% ID/g) and can be cleared rapidly from most tissues. Dynamic scan and pharmacokinetic studies using BGC823-xenograft-bearing mice revealed that [18F]FBQ-C2 accumulates specifically in tumors, with a longer half-life (101.18 ± 6.50 min) in tumor tissues than in other tissues (52.70 ± 12.44 min in muscle). Biodistribution exhibits a high tumor-to-normal tissue ratio (4.8 ± 1.7 for the muscle, 2.5 ± 1.0 for the stomach, 2.2 ± 0.9 for the liver, and 17.8 ± 8.4 for the brain). In conclusion, [18F]FBQ-C2 can be used to perform high-contrast Gln imaging of tumors and can serve as a PET tracer for clin. research. The experimental process involved the reaction of Methyl 6-chloro-6-oxohexanoate(cas: 35444-44-1).Reference of Methyl 6-chloro-6-oxohexanoate
The Article related to fluorine 18 glutamine preparation stability tumor pet imaging, boramino acid, glutamine, in vivo stability, positron emission tomography, Radiation Biochemistry: Disease Diagnosis and Therapy and other aspects.Reference of Methyl 6-chloro-6-oxohexanoate
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