| 19926484 |
Mavel S, Meheux N, Guilloteau D, Emond P: Synthesis and in vitro evaluation of fluorinated diphenyloxide derivatives and sulfur analogs as serotonin transporter ligands. Bioorg Med Chem. 2010 Jan 1;18(1):236-41. Epub 2009 Nov 4.
As the serotonin transporter (SERT) is involved in several neurodegenerative and psychiatric disorders; radiopharmaceuticals to image the SERT by PET would be valuable in studying these diseases. To this end we synthesized diphenyloxide derivatives and sulfide analogs, as new tracers, incorporating a fluorine or oxyalkyl fluorinated group on 4' or 5'-position on phenyl ring B. Three of these exhibited good to high in vitro affinity (7 <8 nM) and selectivity for the SERT over the other monoamine transporters. |
83(1,1,1,3) |