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

Nucl Med Biol. 2003 Jul;30(5):477-90. doi: 10.1016/s0969-8051(03)00025-8.

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.

Publication types

  • Comparative Study
  • Evaluation Study
  • Validation Study

MeSH terms

  • Amino Acids / chemical synthesis
  • Amino Acids / pharmacokinetics
  • Aminobutyrates / chemical synthesis
  • Aminobutyrates / pharmacokinetics*
  • Animals
  • Brain Neoplasms / diagnostic imaging*
  • Brain Neoplasms / metabolism*
  • Cell Line, Tumor
  • Fluorine Radioisotopes / chemistry
  • Fluorine Radioisotopes / pharmacokinetics
  • Gliosarcoma / diagnostic imaging*
  • Gliosarcoma / metabolism*
  • Isotope Labeling / methods*
  • Male
  • Metabolic Clearance Rate
  • Neoplasm Transplantation
  • Organ Specificity
  • Radionuclide Imaging
  • Radiopharmaceuticals / chemical synthesis
  • Radiopharmaceuticals / metabolism
  • Radiopharmaceuticals / pharmacokinetics
  • Rats
  • Rats, Inbred F344
  • Reference Values
  • Tissue Distribution

Substances

  • 2-amino-4-fluoro-2-methylbutanoic acid
  • Amino Acids
  • Aminobutyrates
  • Fluorine Radioisotopes
  • Radiopharmaceuticals