Synthesis and biological evaluation of anti-1-amino-2-[18F]fluoro-cyclobutyl-1-carboxylic acid (anti-2-[18F]FACBC) in rat 9L gliosarcoma.
A new [(18)F] labeled amino acid anti-1-amino-2-[(18)F]fluoro-cyclobutyl-1-carboxylic acid 9 (anti-2-[(18)F]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 [(18)F]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 [(18)F]9 had a rapid and prolonged accumulation in tumors with 26:1 tumor to brain ratio at 120 min post-injection. In this model, [(18)F]9 is a potential PET tracer for brain tumor imaging.
Yu
Weiping
W
Department of Radiology, School of Medicine, Emory University, Atlanta, GA 30322, USA.
Williams
Larry
L
Camp
Vernon M
VM
Olson
Jeffrey J
JJ
Goodman
Mark M
MM
D000818:Animals; D001921:Brain / Q000378:metabolism; D002264:Carboxylic Acids / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D045744:Cell Line, Tumor; D002463:Cell Membrane Permeability; D003503:Cyclobutanes / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D005462:Fluorine Radioisotopes / Q000737:chemistry / Q000493:pharmacokinetics; D018316:Gliosarcoma / Q000000981:diagnostic imaging*; D008297:Male; D049268:Positron-Emission Tomography / Q000379:methods*; D051381:Rats; D011916:Rats, Inbred F344
D002264:Carboxylic Acids; D003503:Cyclobutanes; D005462:Fluorine Radioisotopes; C117460:fluciclovine F-18