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      Docking study, synthesis, and in vitro evaluation of fluoro-MADAM derivatives as SERT ligands for PET imaging.

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          Abstract

          In order to predict affinity of new diphenylsulfides for the serotonin transporter (SERT), a molecular modeling model was used to compare potential binding affinity of new compounds with known potent ligands. The aim of this study is to identify a suitable PET radioligand for imaging the SERT, new derivatives, and their precursors for a C-11 or F-18 radiolabeling, were synthesized. Two fluorinated derivatives displayed good in vitro affinity for the SERT (K(i)=14.3+/-1 and 10.1+/-2.7 nM) and good selectivity toward the other monoamine transporters as predicted by the docking study.

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          Author and article information

          Journal
          Bioorg. Med. Chem.
          Bioorganic & medicinal chemistry
          Elsevier BV
          1464-3391
          0968-0896
          Oct 01 2008
          : 16
          : 19
          Affiliations
          [1 ] INSERM U930, 37000 TOURS, France; Université François-Rabelais de Tours, 37000 TOURS, France. sylvie.mavel@univ-tours.fr
          Article
          S0968-0896(08)00718-9
          10.1016/j.bmc.2008.08.002
          18793858
          db0d2aad-adfc-4349-9ec0-113fd567c974
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