Improved radiosynthesis and preliminary in vivo evaluation of the 11 C-labeled tetrazine [ 11 C]AE-1 for pretargeted PET imaging
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- OA-Improved radiosynthesis and preliminary in vivo evaluation of the 11 C-labeled tetrazine
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Pretargeted nuclear imaging based on the ligation between tetrazines and nano-sized targeting agents functionalized with trans-cyclooctene (TCO) has recently been shown to improve both imaging contrast and dosimetry in nuclear imaging of nanomedicines. Herein, we describe the improved radiosynthesis of a 11 C-labeled tetrazine ([ 11 C]AE-1) and its preliminary evaluation in both mice and pigs. Pretargeted imaging in mice was carried out using both a new TCO-functionalized polyglutamic acid and a previously reported TCO-functionalized bisphosphonate system as targeting agents. Unfortunately, pretargeted imaging was not successful using these targeting agents in pair with [ 11 C]AE-1. However, brain imaging in pig indicated that the tracer crossed the blood-brain-barrier. Hence, we suggest that this tetrazine scaffold could be used as a starting point for the development of pretargeted brain imaging, which has so far been a challenging task.
Original language | English |
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Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 29 |
Issue number | 8 |
Pages (from-to) | 986-990 |
ISSN | 0960-894X |
DOIs | |
Publication status | Published - 1 Jan 2019 |
- Carbon-11, PET imaging, Pretargeting, Tetrazine, Trans-cyclooctene
Research areas
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