Evaluation of Organo [18F]Fluorosilicon Tetrazine as a Prosthetic Group for the Synthesis of PET Radiotracers

• Published in: Molecules (Basel, Switzerland) Vol. 25; no. 5; p. 1208
• Main Authors: Otaru, Sofia, Imlimthan, Surachet, Sarparanta, Mirkka, Helariutta, Kerttuli, Wähälä, Kristiina, Airaksinen, Anu
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 07.03.2020; MDPI
• Subjects: Animals; bioorthogonal chemistry; Blood Proteins - metabolism; Cycloaddition Reaction; Cyclooctanes - chemistry; Drug Stability; Female; Fluorides; Fluorine; Fluorine Radioisotopes - chemistry; Fluorine Radioisotopes - pharmacokinetics; fluorine-18; Humans; inverse electron-demand diels-alder ligation; Investigations; isotopic exchange; Magnetic Resonance Spectroscopy; Mice; Nanoparticles; positron emission tomography (pet), defluorination; Positron-Emission Tomography - methods; Prostheses; Radiopharmaceuticals - chemical synthesis; Radiopharmaceuticals - chemistry; Radiopharmaceuticals - pharmacokinetics; Serum Albumin, Bovine - chemistry; Silicon - chemistry; silicon-based fluoride acceptor; tetrazine; Tissue Distribution; isotopic exchange; positron emission tomography (PET), defluorination; fluorine-18; silicon-based fluoride acceptor; inverse electron-demand Diels-Alder ligation; bioorthogonal chemistry; tetrazine

Fluorine-18 is the most widely used positron emission tomography (PET) radionuclide currently in clinical application, due to its optimal nuclear properties. The synthesis of 18F-labeled radiotracers often requires harsh reaction conditions, limiting the use of sensitive bio- and macromolecules as p...