Title
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Automated one-step radiosynthesis of the CB1 receptor imaging agent []MK-9470
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Author
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Abstract
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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. |
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Language
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Dutch
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Source (journal)
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Journal of labelled compounds and radiopharmaceuticals. - New York
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Publication
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New York
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2014
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ISSN
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0362-4803
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DOI
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10.1002/JLCR.3219
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Volume/pages
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57
:10
(2014)
, p. 611-614
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ISI
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000342834100004
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Full text (Publisher's DOI)
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Full text (publisher's version - intranet only)
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