Synthesis and evaluation of 2-amino-4-[(18)F]fluoro-2-methylbutanoic acid (FAMB): relationship of amino acid transport to tumor imaging properties of branched fluorinated amino acids.

Academic Article

Abstract

  • Radiolabeled amino acids represent a promising class of tumor imaging agents, and the determination of the optimal characteristics of these tracers remains an area of active investigation. A new (18)F-labeled branched amino acid, 2-amino-4-[(18)F]fluoro-2-methylbutanoic acid (FAMB), has been prepared in 36% decay-corrected yield using no-carrier-added [(18)F]fluoride. In vitro uptake assays with rat 9L gliosarcoma cells suggest that [(18)F]FAMB was transported primarily via the L type amino acid transport system. In vivo studies with [(18)F]FAMB demonstrated tumor to normal brain ratios of 14:1 in rats with intracranial 9L gliosarcoma tumors at 60 minutes after injection. Comparison of [(18)F]FAMB with structurally related (18)F-labeled branched amino acids demonstrated that A type transport in vitro was positively correlated with the tumor to brain ratios observed in vivo.
  • Published In

    Keywords

  • Amino Acids, Aminobutyrates, Animals, Brain Neoplasms, Cell Line, Tumor, Fluorine Radioisotopes, Gliosarcoma, Isotope Labeling, Male, Metabolic Clearance Rate, Neoplasm Transplantation, Organ Specificity, Radionuclide Imaging, Radiopharmaceuticals, Rats, Rats, Inbred F344, Reference Values, Tissue Distribution
  • Digital Object Identifier (doi)

    Pubmed Id

  • 23050716
  • Author List

  • McConathy J; Martarello L; Malveaux EJ; Camp VM; Simpson NE; Simpson CP; Bowers GD; Zhang Z; Olson JJ; Goodman MM
  • Start Page

  • 477
  • End Page

  • 490
  • Volume

  • 30
  • Issue

  • 5