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Synthesis of 2'-Deoxy-2'-[(18)F]Fluoro-9-β-D: -Arabinofuranosylguanine: a Novel Agent for Imaging T-Cell Activation with PET.
MedLine Citation:
PMID:  20838911     Owner:  NLM     Status:  In-Data-Review    
Abstract/OtherAbstract:
PURPOSE: 9-(β-D: -Arabinofuranosyl)guanine (AraG) is a guanosine analog that has a proven efficacy in the treatment of T-cell lymphoblastic disease. To test the possibility of using a radiofluorinated AraG as an imaging agent, we have synthesized 2'-deoxy-2'-[(18)F]fluoro-9-β-D: -arabinofuranosylguanine ([(18)F]F-AraG) and investigated its uptake in T cells.
PROCEDURE: We have synthesized [(18)F]F-AraG via a direct fluorination of 2-N-acetyl-6-O-((4-nitrophenyl)ethyl)-9-(3',5'-di-O-trityl-2'-O-trifyl-β-D: -ribofuranosyl)guanine with [(18)F]KF/K.2.2.2 in DMSO at 85°C for 45 min. [(18)F]F-AraG uptake in both a CCRF-CEM leukemia cell line (unactivated) and activated primary thymocytes was evaluated.
RESULTS: We have successfully prepared [(18)F]F-AraG in 7-10% radiochemical yield (decay corrected) with a specific activity of 0.8-1.3 Ci/μmol. Preliminary cell uptake experiments showed that both a CCRF-CEM leukemia cell line and activated primary thymocytes take up the [(18)F]F-AraG.
CONCLUSION: For the first time to the best of our knowledge, [(18)F]F-AraG has been successfully synthesized by direct fluorination of an appropriate precursor of a guanosine nucleoside. This approach maybe also useful for the synthesis of other important positron emission tomography (PET) probes such as [(18)F]FEAU, [(18)F]FMAU, and [(18)F]FBAU which are currently synthesized by multiple steps and involve lengthy purification. The cell uptake studies support future studies to investigate the use of [(18)F]F-AraG as a PET imaging agent of T cells.
Authors:
Mohammad Namavari; Ya-Fang Chang; Brenda Kusler; Shahriar Yaghoubi; Beverly S Mitchell; Sanjiv Sam Gambhir
Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Molecular imaging and biology : MIB : the official publication of the Academy of Molecular Imaging     Volume:  13     ISSN:  1860-2002     ISO Abbreviation:  Mol Imaging Biol     Publication Date:  2011 Oct 
Date Detail:
Created Date:  2011-09-28     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101125610     Medline TA:  Mol Imaging Biol     Country:  United States    
Other Details:
Languages:  eng     Pagination:  812-8     Citation Subset:  IM    
Affiliation:
Molecular Imaging Program at Stanford (MIPS), Stanford University, 318 Campus Dr., Clark Center, E-150, Stanford, CA, 94305, USA.
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