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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).
- Source :
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Journal of medicinal chemistry [J Med Chem] 2016 Oct 13; Vol. 59 (19), pp. 8955-8966. Date of Electronic Publication: 2016 Sep 20. - Publication Year :
- 2016
-
Abstract
- We herein describe the straightforward synthesis of a stable pyridyl(4-methoxyphenyl)iodonium salt and its [ <superscript>18</superscript> F] radiolabeling within a one-step, fully automated and cGMP compliant radiosynthesis of [ <superscript>18</superscript> F]UCB-H ([ <superscript>18</superscript> 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 [ <superscript>18</superscript> F]7 from up to 285 GBq (7.7 Ci) of [ <superscript>18</superscript> 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 [ <superscript>18</superscript> 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 cGMP <superscript>18</superscript> F-PET tracer manufacturing industry, and their ability to fulfill practical and regulatory requirements in that field.
- 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
Subjects
Details
- Language :
- English
- ISSN :
- 1520-4804
- Volume :
- 59
- Issue :
- 19
- Database :
- MEDLINE
- Journal :
- Journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 27598384
- Full Text :
- https://doi.org/10.1021/acs.jmedchem.6b00905