1 research outputs found
Design, Synthesis, and Evaluation of a Low-Molecular-Weight <sup>11</sup>C‑Labeled Tetrazine for Pretargeted PET Imaging Applying Bioorthogonal in Vivo Click Chemistry
A low-molecular-weight
tetrazine labeled with the short-lived positron
emitter carbon-11 was developed as a bioorthogonal PET probe for pretargeted
imaging. A method for efficient and fast synthesis of this imaging
agent is presented using radiolabeling of a readily available precursor.
High reactivity with <i>trans</i>-cyclooctenes was observed
and in vivo investigations including PET/MR scanning showed homogeneous
biodistribution, good metabolic stability, and rapid excretion in
naive mice. These properties are key to the success of bioorthogonal <sup>11</sup>C-PET imaging, which has been shown in a simple pretargeting
experiment using TCO-modified mesoporous silica nanoparticles. Overall,
this <sup>11</sup>C-labeled tetrazine represents a highly versatile
and advantageous chemical tool for bioorthogonal PET imaging and enables
pretargeting approaches using carbon-11 for the first time