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Synthesis and in vitro evaluation of fluorinated diphenyloxide derivatives and sulfur analogs as serotonin transporter ligands.

Authors :
Mavel S
Meheux N
Guilloteau D
Emond P
Source :
Bioorganic & medicinal chemistry [Bioorg Med Chem] 2010 Jan 01; Vol. 18 (1), pp. 236-41. Date of Electronic Publication: 2009 Nov 04.
Publication Year :
2010

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<K(i)<8 nM) and selectivity for the SERT over the other monoamine transporters.<br /> (Copyright (c) 2009 Elsevier Ltd. All rights reserved.)

Details

Language :
English
ISSN :
1464-3391
Volume :
18
Issue :
1
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry
Publication Type :
Academic Journal
Accession number :
19926484
Full Text :
https://doi.org/10.1016/j.bmc.2009.10.062