Evaluation of F-537-Tetrazine in a model for brain pretargeting imaging. Comparison to N-(3-[18F] fluoro-5-(1,2,4,5-tetrazin-3-yl)benzyl)propan-1-amine

• Published in: Nuclear medicine and biology Vol. 128-129; p. 108877
• Main Authors: Shalgunov, Vladimir, van den Broek, Sara Lopes, Andersen, Ida Vang, Raval, Nakul R., Schäfer, Gabriela, Barz, Matthias, Herth, Matthias M., Battisti, Umberto M.
• Format: Journal Article
• Language: English
• Published: United States Elsevier Inc 01.01.2024
• Subjects: Blood-brain-barrier; Imaging; Pretargeting; Tetrazine ligation; Blood-brain-barrier; Tetrazine ligation; Imaging; Pretargeting
• ISSN: 0969-8051; 1872-9614; 1872-9614
• DOI: 10.1016/j.nucmedbio.2024.108877

Brain pretargeted nuclear imaging for the diagnosis of various neurodegenerative diseases is a quickly developing field. The tetrazine ligation is currently the most explored approach to achieve this goal due to its remarkable properties. In this work, we evaluated the performance of F-537-Tetrazine, previously developed by Biogen, and N-(3-[18F]fluoro-5-(1,2,4,5-tetrazin-3-yl)benzyl)propan-1-amine, previously developed in our group, thereby allowing for the direct comparison of these two imaging probes. The evaluation included synthesis, radiolabeling and a comparison of the physicochemical properties of the compounds. Furthermore, their performance was evaluated by in vitro and in vivo pretargeting models. This study indicated that N-(3-[18F] fluoro-5-(1,2,4,5-tetrazin-3-yl)benzyl)propan-1-amine might be more suited for brain pretargeted imaging. [Display omitted]