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Automated one-step radiosynthesis of the CB1 receptor imaging agent [$^{18}F$]MK-9470

Tijdschriftbijdrage - Tijdschriftartikel

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.
Tijdschrift: Journal of labelled compounds and radiopharmaceuticals
ISSN: 0362-4803
Volume: 57
Pagina's: 611 - 614
Jaar van publicatie:2014
Trefwoorden:A1 Journal article
Toegankelijkheid:Closed