Synthesis and biological evaluation of anti-1-amino-2-[F-18]fluoro-cyclobutyl-1-carboxylic acid (anti-2-[F-18]FACBC) in rat 9L gliosarcoma

A new [F-18] labeled amino acid anti-1-amino-2-[F-18] fluoro-cyclobutyl-1-carboxylic acid 9 (anti-2[F-18] 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 [F-18]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 [F-18]9 had a rapid and prolonged accumulation in tumors with 26: 1 tumor to brain ratio at 120 min post-injection. In this model, [F-18] 9 is a potential PET tracer for brain tumor imaging. (C) 2010 Elsevier Ltd. All rights reserved.