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Automated one-step radiosynthesis of the CB1receptor imaging agent [18F]MK-9470
- Source :
- Journal of Labelled Compounds and Radiopharmaceuticals. 57:611-614
- Publication Year :
- 2014
- Publisher :
- Wiley, 2014.
-
Abstract
- The fluorine-18-labeled positron emission tomography (PET) radiotracer [(18) F]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 [(18) F]radiofluorination approach using a GE TRACERlab FXFN module for the routine production of this tracer. The one-step synthesis, by [(18) F]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-[(18) F]fluorobromoethane. The average radiochemical yield of [(18) F]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 [(18) F]MK-9470 for clinical studies.
- Subjects :
- Cannabinoid receptor
medicine.diagnostic_test
Chemistry
Organic Chemistry
Radiosynthesis
Radiochemistry
Analytical chemistry
One-Step
Biochemistry
Imaging agent
Analytical Chemistry
Positron emission tomography
Yield (chemistry)
Drug Discovery
medicine
Inverse agonist
Radiology, Nuclear Medicine and imaging
Specific activity
Spectroscopy
Subjects
Details
- ISSN :
- 03624803
- Volume :
- 57
- Database :
- OpenAIRE
- Journal :
- Journal of Labelled Compounds and Radiopharmaceuticals
- Accession number :
- edsair.doi...........f9678df46a3fb586d1711afbde5d6fb1