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.
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.
McConathy
Jonathan
J
Department of Radiology, Emory University, Atlanta, GA 30322, USA.
Martarello
Laurent
L
Malveaux
Eugene J
EJ
Camp
Vernon M
VM
Simpson
Nicholas E
NE
Simpson
Chiab P
CP
Bowers
Geoffrey D
GD
Zhang
Zhaobin
Z
Olson
Jeffrey J
JJ
Goodman
Mark M
MM
D000596:Amino Acids / Q000138:chemical synthesis / Q000493:pharmacokinetics; D000613:Aminobutyrates / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D000818:Animals; D001932:Brain Neoplasms / Q000000981:diagnostic imaging* / Q000378:metabolism*; D045744:Cell Line, Tumor; D005462:Fluorine Radioisotopes / Q000737:chemistry / Q000493:pharmacokinetics; D018316:Gliosarcoma / Q000000981:diagnostic imaging* / Q000378:metabolism*; D007553:Isotope Labeling / Q000379:methods*; D008297:Male; D008657:Metabolic Clearance Rate; D009368:Neoplasm Transplantation; D009928:Organ Specificity; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000378:metabolism / Q000493:pharmacokinetics; D051381:Rats; D011916:Rats, Inbred F344; D012016:Reference Values; D014018:Tissue Distribution
C483763:2-amino-4-fluoro-2-methylbutanoic acid; D000596:Amino Acids; D000613:Aminobutyrates; D005462:Fluorine Radioisotopes; D019275:Radiopharmaceuticals