Synthesis and in vitro evaluation of fluorinated diphenyloxide derivatives and sulfur analogs as serotonin transporter ligands.
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<K(i)<8 nM) and selectivity for the SERT over the other monoamine transporters.
Mavel
Sylvie
S
Université François Rabelais de Tours, INSERM U930, 37000 TOURS, France. sylvie.mavel@univ-tours.fr
Meheux
Nathalie
N
Guilloteau
Denis
D
Emond
Patrick
P
D001667:Binding, Competitive; D045744:Cell Line, Tumor; D050483:Dopamine Plasma Membrane Transport Proteins / Q000378:metabolism; D054879:Halogenation; D006801:Humans; D008024:Ligands; D050484:Norepinephrine Plasma Membrane Transport Proteins / Q000378:metabolism; D010647:Phenyl Ethers / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D050486:Serotonin Plasma Membrane Transport Proteins / Q000378:metabolism*; D013440:Sulfides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
D050483:Dopamine Plasma Membrane Transport Proteins; D008024:Ligands; D050484:Norepinephrine Plasma Membrane Transport Proteins; D010647:Phenyl Ethers; C493227:SLC6A2 protein, human; D050486:Serotonin Plasma Membrane Transport Proteins; D013440:Sulfides