Synthesis and biological evaluation of anti-1-amino-2-[18F]fluoro-cyclobutyl-1-carboxylic acid (anti-2-[18F]FACBC) in rat 9L gliosarcoma |
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| Authors: | Weiping Yu Larry Williams Vernon M. Camp Jeffrey J. Olson Mark M. Goodman |
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| Affiliation: | 1. Department of Radiology, School of Medicine, Emory University, Atlanta, GA 30322, USA;2. Department of Neurosurgery, School of Medicine, Emory University, Atlanta, GA 30322, USA |
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| Abstract: | A new [18F] labeled amino acid anti-1-amino-2-[18F]fluoro-cyclobutyl-1-carboxylic acid 9 (anti-2-[18F]FACBC) was synthesized in 30% decay-corrected yield with high radiochemical purity over 99%. The cyclic sulfamidate precursor was very stable and highly reactive towards nucleophilic radiofluorination. Cell uptake assays with rat 9L gliosarcoma cells showed that [18F]9 was transported into tumor cells via multiple amino acid transport systems, including L and A systems. Biodistribution study in rats with intracranial 9L gliosarcoma tumors demonstrated that [18F]9 had a rapid and prolonged accumulation in tumors with 26:1 tumor to brain ratio at 120 min post-injection. In this model, [18F]9 is a potential PET tracer for brain tumor imaging. |
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