A novel approach to the synthesis of [18F]flumazenil, a radioligand for PET imaging of central benzodiazepine receptors
- Authors: Nasirzadeh M.1, Vaulina D.D.2, Kuznetsova O.F.2, Gomzina N.A.2
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Affiliations:
- Institute of Chemistry, St. Petersburg State University
- N. P. Bechtereva Institute of Human Brain, Russian Academy of Sciences
- Issue: Vol 65, No 3 (2016)
- Pages: 794-800
- Section: Full Articles
- URL: https://journals.rcsi.science/1066-5285/article/view/237665
- DOI: https://doi.org/10.1007/s11172-016-1376-1
- ID: 237665
Cite item
Abstract
An express method of solid-phase extraction was proposed for the first time for isolation and purification of [18F]flumazenil, a radioligand used to quantify the density of central benzodiazepine receptors by positron emission tomography (PET). This novel approach afforded the radioligand with >97% radiochemical purity and a high chemical purity (nitromazenil content <1 μg mL–1) and considerably reduced the time of the synthesis (from 90 to 50 min). The nonoptimized decay-corrected radiochemical yield was 8%, and the specific radioactivity was >37 GBq μmol–1. The novel synthetic procedure easily can be integrated into automatic modules for the synthesis of clinically used PET radiopharmaceuticals.
About the authors
M. Nasirzadeh
Institute of Chemistry, St. Petersburg State University
Email: gomzina@ihb.spb.ru
Russian Federation, 7—9 Universitetskaya nab., St. Petersburg, 199034
D. D. Vaulina
N. P. Bechtereva Institute of Human Brain, Russian Academy of Sciences
Email: gomzina@ihb.spb.ru
Russian Federation, 9 ul. Akad. Pavlova, St. Petersburg, 197376
O. F. Kuznetsova
N. P. Bechtereva Institute of Human Brain, Russian Academy of Sciences
Email: gomzina@ihb.spb.ru
Russian Federation, 9 ul. Akad. Pavlova, St. Petersburg, 197376
N. A. Gomzina
N. P. Bechtereva Institute of Human Brain, Russian Academy of Sciences
Author for correspondence.
Email: gomzina@ihb.spb.ru
Russian Federation, 9 ul. Akad. Pavlova, St. Petersburg, 197376