1083194-30-2Relevant academic research and scientific papers
Docking study, synthesis, and in vitro evaluation of fluoro-MADAM derivatives as SERT ligands for PET imaging
Mavel, Sylvie,Vercouillie, Johnny,Garreau, Lucette,Raguza, Tiziana,Ravna, Aina Westrheim,Chalon, Sylvie,Guilloteau, Denis,Emond, Patrick
, p. 9050 - 9055 (2008/12/23)
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 (Ki = 14.3 ± 1 and 10.1 ± 2.7 nM) and good selectivity toward the other monoamine transporters as predicted by the docking study.
