Research
Print page Print page
Switch language
The Capital Region of Denmark - a part of Copenhagen University Hospital
Published

Improved radiosynthesis and preliminary in vivo evaluation of the 11C-labeled tetrazine [11C]AE-1 for pretargeted PET imaging

Research output: Contribution to journalJournal articleResearchpeer-review

  1. Labeling and preliminary in vivo evaluation of the 5-HT(7) receptor selective agonist [(11)C]E-55888

    Research output: Contribution to journalJournal articleResearchpeer-review

  2. (11)C-labeling and preliminary evaluation of pimavanserin as a 5-HT2A receptor PET-radioligand

    Research output: Contribution to journalJournal articleResearchpeer-review

  3. (11)C-labeling and preliminary evaluation of vortioxetine as a PET radioligand

    Research output: Contribution to journalJournal articleResearchpeer-review

  4. Synthesis, in vitro and in vivo evaluation of [11C]MMTP: a potential PET ligand for mGluR1 receptors

    Research output: Contribution to journalJournal articleResearchpeer-review

View graph of relations

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 11C-labeled tetrazine ([11C]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 [11C]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 & Medicinal Chemistry Letters
Volume29
Issue number8
Pages (from-to)986-990
Number of pages5
ISSN0960-894X
DOIs
Publication statusPublished - 15 Apr 2019

    Research areas

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

ID: 56670503