1. Enabling Efficient Positron Emission Tomography (PET) Imaging of Synaptic Vesicle Glycoprotein 2A (SV2A) with a Robust and One-Step Radiosynthesis of a Highly Potent 18 F-Labeled Ligand ([ 18 F]UCB-H).
- Author
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Warnier C, Lemaire C, Becker G, Zaragoza G, Giacomelli F, Aerts J, Otabashi M, Bahri MA, Mercier J, Plenevaux A, and Luxen A
- Subjects
- Animals, Male, Models, Molecular, Pyridines chemical synthesis, Pyrrolidinones chemical synthesis, Rats, Rats, Sprague-Dawley, Fluorine Radioisotopes chemistry, Membrane Glycoproteins analysis, Nerve Tissue Proteins analysis, Positron-Emission Tomography methods, Pyridines chemistry, Pyrrolidinones chemistry
- Abstract
We herein describe the straightforward synthesis of a stable pyridyl(4-methoxyphenyl)iodonium salt and its [
18 F] radiolabeling within a one-step, fully automated and cGMP compliant radiosynthesis of [18 F]UCB-H ([18 F]7), a PET tracer for the imaging of synaptic vesicle glycoprotein 2A (SV2A). Over the course of 1 year, 50 automated productions provided 34 ± 2% of injectable [18 F]7 from up to 285 GBq (7.7 Ci) of [18 F]fluoride in 50 min (uncorrected radiochemical yield, specific activity of 815 ± 185 GBq/μmol). The successful implementation of our synthetic strategy within routine, high-activity, and cGMP productions attests to its practicality and reliability for the production of large doses of [18 F]7. In addition to enabling efficient and cost-effective clinical research on a range of neurological pathologies through the imaging of SV2A, this work further demonstrates the real value of iodonium salts for the cGMP18 F-PET tracer manufacturing industry, and their ability to fulfill practical and regulatory requirements in that field.- Published
- 2016
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