Synthesis and in vitro evaluation of fluorinated diphenyloxide derivatives and sulfur analogs as serotonin transporter ligands Original Research Article

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 < Ki < 8 nM) and selectivity for the SERT over the other monoamine transporters.