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

作者：Thomae David; Morley Thomas J^*; Hamill Terence; Carroll Vincent M; Papin Caroline; Twardy Nicole M; Lee H Sharon; Hargreaves Richard; Baldwin Ronald M; Tamagnan Gilles; Alagille David

来源：Journal of Labelled Compounds and Radiopharmaceuticals, 2014, 57(10): 611-614.

DOI：10.1002/jlcr.3219

• [18F]MK-9470
• CB1
• Production
• Good Manufacturing Practice (GMP)

The fluorine-18-labeled positron emission tomography (PET) radiotracer [F-18]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 [F-18]radiofluorination approach using a GE TRACERlab FXFN module for the routine production of this tracer. The one-step synthesis, by [F-18]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-[F-18]fluorobromoethane. The average radiochemical yield of [F-18]MK-9470 using the one-step method was 30.3 +/- 11.7% (n=12), with specific activity in excess of 6Ci/mu mol and radiochemical purity of 97.2 +/- 1.5% (n=12), in less than 60min. This simplified, high yielding, automated process was validated for routine GMP production of [F-18]MK-9470 for clinical studies.

• 出版日期2014-8