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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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 languageEnglish
JournalBioorganic and Medicinal Chemistry Letters
Issue number8
Pages (from-to)986-990
Publication statusPublished - 1 Jan 2019

    Research areas

  • Carbon-11, PET imaging, Pretargeting, Tetrazine, Trans-cyclooctene

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