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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
Nuclear Medicine and Biology ( IF 3.6 ) Pub Date : 2024-01-11 , DOI: 10.1016/j.nucmedbio.2024.108877 Vladimir Shalgunov 1 , Sara Lopes van den Broek 1 , Ida Vang Andersen 1 , Nakul R Raval 2 , Gabriela Schäfer 3 , Matthias Barz 3 , Matthias M Herth 4 , Umberto M Battisti 1
Nuclear Medicine and Biology ( IF 3.6 ) Pub Date : 2024-01-11 , DOI: 10.1016/j.nucmedbio.2024.108877 Vladimir Shalgunov 1 , Sara Lopes van den Broek 1 , Ida Vang Andersen 1 , Nakul R Raval 2 , Gabriela Schäfer 3 , Matthias Barz 3 , Matthias M Herth 4 , Umberto M Battisti 1
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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-[F]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-[F] fluoro-5-(1,2,4,5-tetrazin-3-yl)benzyl)propan-1-amine might be more suited for brain pretargeted imaging.
中文翻译：
F-537-四嗪在大脑预靶向成像模型中的评估。与 N-(3-[18F] 氟-5-(1,2,4,5-四嗪-3-基)苄基)丙-1-胺的比较
用于诊断各种神经退行性疾病的脑预靶向核成像是一个快速发展的领域。由于其卓越的特性，四嗪连接是目前实现这一目标的探索最多的方法。在这项工作中，我们评估了 Biogen 先前开发的 F-537-四嗪和 N-(3-[F]氟-5-(1,2,4,5-四嗪-3-基)苄基) 的性能propan-1-amine，我们小组之前开发的，因此可以直接比较这两种成像探针。评估包括化合物的合成、放射性标记和理化性质的比较。此外，通过体外和体内预靶向模型评估了它们的性能。这项研究表明，N-(3-[F] 氟-5-(1,2,4,5-四嗪-3-基)苯甲基)丙-1-胺可能更适合大脑预靶向成像。
更新日期：2024-01-11
中文翻译：
F-537-四嗪在大脑预靶向成像模型中的评估。与 N-(3-[18F] 氟-5-(1,2,4,5-四嗪-3-基)苄基)丙-1-胺的比较
用于诊断各种神经退行性疾病的脑预靶向核成像是一个快速发展的领域。由于其卓越的特性，四嗪连接是目前实现这一目标的探索最多的方法。在这项工作中，我们评估了 Biogen 先前开发的 F-537-四嗪和 N-(3-[F]氟-5-(1,2,4,5-四嗪-3-基)苄基) 的性能propan-1-amine，我们小组之前开发的，因此可以直接比较这两种成像探针。评估包括化合物的合成、放射性标记和理化性质的比较。此外，通过体外和体内预靶向模型评估了它们的性能。这项研究表明，N-(3-[F] 氟-5-(1,2,4,5-四嗪-3-基)苯甲基)丙-1-胺可能更适合大脑预靶向成像。
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