Synthesis and in vitro evaluation of fluorinated diphenyloxide derivatives and sulfur analogs as serotonin transporter ligands |
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Authors: | Sylvie Mavel Nathalie Meheux Denis Guilloteau Patrick Emond |
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Institution: | Université François Rabelais de Tours, INSERM U930, 37000 TOURS, France;CHRU, Hôpital Bretonneau, Service de Médecine Nucléaire, 37000 TOURS, France |
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Abstract: | 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. |
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