Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 5, Pages 1749-1751Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.01.052
Keywords
Glutamate; NMDA; PET; Fluorine-18; Imaging
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Two S-[F-18]fluoroalkylated diarylguanidines were synthesized and evaluated in vitro as potential tracers for imaging of N-methyl-D-aspartate receptors (NMDARs) with positron emission tomography (PET). [F-18]1 and [F-18]10 were synthesized by [F-18]fluoroethylation and [F-18]fluoromethylation of the thiol precursor 6, respectively. [F-18]1 is a promising candidate NMDAR PET tracer, with low nanomolar affinity for the NMDA PCP-site, high selectivity and moderate lipophilicity. (C) 2010 Elsevier Ltd. All rights reserved.
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