NDLI: A New Highly Reactive and Low Lipophilicity Fluorine-18 Labeled Tetrazine Derivative for Pretargeted PET Imaging.

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A New Highly Reactive and Low Lipophilicity Fluorine-18 Labeled Tetrazine Derivative for Pretargeted PET Imaging.

Content Provider	Semantic Scholar
Author	Keinänen, Outi M. Li, Xiang-Guo Chenna, Naveen Kumar Lumen, Dave Ott, Jennifer Molthoff, Carla F. M. Sarparanta, Mirkka Helariutta, Kerttuli Vuorinen, Tapani Windhorst, Albert D. Airaksinen, Anu J.
Copyright Year	2016
Abstract	A new (18)F-labeled tetrazine derivative was developed aiming at optimal radiochemistry, fast reaction kinetics in inverse electron-demand Diels-Alder cycloaddition (IEDDA), and favorable pharmacokinetics for in vivo bioorthogonal chemistry. The radiolabeling of the tetrazine was achieved in high yield, purity, and specific activity under mild reaction conditions via conjugation with 5-[(18)F]fluoro-5-deoxyribose, providing a glycosylated tetrazine derivative with low lipophilicity. The (18)F-tetrazine showed fast reaction kinetics toward the most commonly used dienophiles in IEDDA reactions. It exhibited excellent chemical and enzymatic stability in mouse plasma and in phosphate-buffered saline (pH 7.41). Biodistribution in mice revealed favorable pharmacokinetics with major elimination via urinary excretion. The results indicate that the glycosylated (18)F-labeled tetrazine is an excellent candidate for in vivo bioorthogonal chemistry applications in pretargeted PET imaging approaches.
File Format	PDF HTM / HTML
DOI	10.1021/acsmedchemlett.5b00330
PubMed reference number	26819667
Journal	Medline
Volume Number	7
Issue Number	1
Alternate Webpage(s)	http://wxjs.chinayyhg.com/upload/Files/20160312131934394/2016031213195137.pdf
Alternate Webpage(s)	https://doi.org/10.1021/acsmedchemlett.5b00330
Journal	ACS medicinal chemistry letters
Language	English
Access Restriction	Open
Content Type	Text
Resource Type	Article

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