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

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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 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.


  • Stéen, E Johanna L
  • Jørgensen, Jesper T
  • Petersen, Ida N
  • Nørregaard, Kamilla
  • Lehel, Szabolcs
  • Shalgunov, Vladimir
  • Birke, Alexander
  • Edem, Patricia E
  • L'Estrade, Elina T
  • Hansen, Hanne D
  • Villadsen, Jonas
  • Erlandsson, Maria
  • Ohlsson, Tomas
  • Yazdani, Abdolreza
  • Valliant, John F
  • Kristensen, Jesper L
  • Barz, Matthias
  • Knudsen, Gitte M
  • Kjær, Andreas
  • Herth, Matthias M

publication date

  • April 2019