Document Detail


Synthesis and biological evaluation of anti-1-amino-2-[18F]fluoro-cyclobutyl-1-carboxylic acid (anti-2-[18F]FACBC) in rat 9L gliosarcoma.
MedLine Citation:
PMID:  20207538     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
Weiping Yu; Larry Williams; Vernon M Camp; Jeffrey J Olson; Mark M Goodman
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2010-02-14
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  20     ISSN:  1464-3405     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2010 Apr 
Date Detail:
Created Date:  2010-03-22     Completed Date:  2010-07-05     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  2140-3     Citation Subset:  IM    
Copyright Information:
2010 Elsevier Ltd. All rights reserved.
Affiliation:
Department of Radiology, School of Medicine, Emory University, Atlanta, GA 30322, USA.
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MeSH Terms
Descriptor/Qualifier:
Animals
Brain / metabolism
Carboxylic Acids / chemical synthesis*,  diagnostic use*,  pharmacokinetics
Cell Line, Tumor
Cell Membrane Permeability
Cyclobutanes / chemical synthesis*,  diagnostic use*,  pharmacokinetics
Fluorine Radioisotopes / chemistry,  diagnostic use*,  pharmacokinetics
Gliosarcoma / radionuclide imaging*
Male
Positron-Emission Tomography / methods*
Rats
Rats, Inbred F344
Chemical
Reg. No./Substance:
0/1-amino-3-fluorocyclobutane-1-carboxylic acid; 0/Carboxylic Acids; 0/Cyclobutanes; 0/Fluorine Radioisotopes

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