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http://dx.doi.org/10.22643/JRMP.2022.8.1.3

Automated radiosynthesis for the routine production of [18F]FPEB for imaging metabotropic glutamate receptor 5 (mGluRS)  

Kyung Rok Nam (Division of Applied RI, Korea Institute of Radiological & Medical Sciences)
Sang Jin Han (Division of Applied RI, Korea Institute of Radiological & Medical Sciences)
Kyo Chul Lee (Division of Applied RI, Korea Institute of Radiological & Medical Sciences)
Jae Yong Choi (Division of Applied RI, Korea Institute of Radiological & Medical Sciences)
Publication Information
Journal of Radiopharmaceuticals and Molecular Probes / v.8, no.1, 2022 , pp. 3-8 More about this Journal
Abstract
Alteration of the mGluR5 density is closely related to various brain diseases including schizophrenia, depression, Parkinson's disease, and Alzheimer's disease. Therefore, mGluR5 is considered as a valuable imaging biomarker for brain disease and many radiopharmaceuticals have been developed so far. Among them, [18F]FPEB has favorable pharmacokinetic characteristics, and this is the most frequently used radiopharmaceutical for preclinical and clinical studies. In the present study, we want to introduce the optimized radiosynthetic method for the routine production of [18F]FPEB using a GE TRACERlabTM FXFN pro module. In addition, the entire process was monitored with a webcam to solve the problems arising from the synthetic process. As a result, [18F]FPEB was prepared by nucleophilic substitution from its nitro- precursor at 120℃ for 20 min in dimethyl sulfoxide. Radiochemical yield was 13.7 ± 5.1% (decay-corrected, n = 91) with the molar activity of 84 ± 17 GBq/µmol at the end of synthesis. The radiochemical purity was determined to be above 96%. The manufactured [18F]FPEB injection for quality controls were carried out in accordance with an KIRAMS approved protocol, as per ICH and USP guidelines.
Keywords
$[^{18}F]FPEB$; mGluRS; Brain disease; PET; Automation;
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Times Cited By KSCI : 2  (Citation Analysis)
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