Publication
Title
Automated one-step radiosynthesis of the CB1 receptor imaging agent []MK-9470
Author
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.
Language
Dutch
Source (journal)
Journal of labelled compounds and radiopharmaceuticals. - New York
Publication
New York : 2014
ISSN
0362-4803
Volume/pages
57:10(2014), p. 611-614
ISI
000342834100004
Full text (Publisher's DOI)
Full text (publisher's version - intranet only)
UAntwerpen
Faculty/Department
Research group
[E?say:metaLocaldata.cgzprojectinf]
Publication type
Subject
External links
Web of Science
Record
Identification
Creation 06.11.2014
Last edited 05.11.2017