Title
Automated one-step radiosynthesis of the CB1 receptor imaging agent [<tex>$^{18}F$</tex>]MK-9470 Automated one-step radiosynthesis of the CB1 receptor imaging agent [<tex>$^{18}F$</tex>]MK-9470
Author
Faculty/Department
Faculty of Pharmaceutical, Biomedical and Veterinary Sciences. Pharmacy
Publication type
article
Publication
New York ,
Subject
Biology
Human medicine
Source (journal)
Journal of labelled compounds and radiopharmaceuticals. - New York
Volume/pages
57(2014) :10 , p. 611-614
ISSN
0362-4803
Carrier
E
Target language
Dutch (dut)
Full text (Publishers DOI)
Abstract
The fluorine-18-labeled positron emission tomography (PET) radiotracer [18F]MK-9470 is a selective, high affinity inverse agonist that has been used to image the cannabinoid receptor type 1 in human brain in healthy and disease states. This report describes a simplified, one-step [18F]radiofluorination approach using a GE TRACERlab FXFN module for the routine production of this tracer. The one-step synthesis, by [18F]fluoride displacement of a primary tosylate precursor, gives a six-fold increase in yield over the previous two-step method employing O-alkylation of a phenol precursor with 1,2-[18F]fluorobromoethane. The average radiochemical yield of [18F]MK-9470 using the one-step method was 30.3 ± 11.7% (n = 12), with specific activity in excess of 6 Ci/µmol and radiochemical purity of 97.2 ± 1.5% (n = 12), in less than 60 min. This simplified, high yielding, automated process was validated for routine GMP production of [18F]MK-9470 for clinical studies.
E-info
https://repository.uantwerpen.be/docman/iruaauth/fda60c/24735aaa358.pdf