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

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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-[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.

OriginalsprogEngelsk
Artikelnummer108877
TidsskriftNuclear Medicine and Biology
Vol/bind128-129
Antal sider12
ISSN0969-8051
DOI
StatusUdgivet - 2024

Bibliografisk note

Funding Information:
Stina Syvänen and Dag Sehlin (Uppsala University) are acknowledged for kindly providing the 3D6 antibody and the tg-ArcSwe brain tissue. This project has received funding from the European Union's EU Framework Programme for Research and Innovation Horizon 2020 , under grant agreement no. 668532 . MMH has received funding from the European Union's EU Framework Programme for Research and Innovation Horizon 2020 (grant agreement no. 670261 ). VS was supported by BRIDGE – Translational Excellence Programme at the Faculty of Health and Medical Sciences, University of Copenhagen , funded by the Novo Nordisk Foundation (grant agreement no. NNF18SA0034956 ). The Lundbeck Foundation , the Novo Nordisk Foundation , the Innovation Fund Denmark , and the Research Council for Independent Research (grant agreement no. 8022-00187B ) are further acknowledged.

Funding Information:
Stina Syvänen and Dag Sehlin (Uppsala University) are acknowledged for kindly providing the 3D6 antibody and the tg-ArcSwe brain tissue. This project has received funding from the European Union's EU Framework Programme for Research and Innovation Horizon 2020, under grant agreement no. 668532. MMH has received funding from the European Union's EU Framework Programme for Research and Innovation Horizon 2020 (grant agreement no. 670261). VS was supported by BRIDGE – Translational Excellence Programme at the Faculty of Health and Medical Sciences, University of Copenhagen, funded by the Novo Nordisk Foundation (grant agreement no. NNF18SA0034956). The Lundbeck Foundation, the Novo Nordisk Foundation, the Innovation Fund Denmark, and the Research Council for Independent Research (grant agreement no. 8022-00187B) are further acknowledged.

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© 2024 The Authors

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