title: Synthesis and in vitro evaluation of novel derivatives of diphenylsulfide as serotonin transporter ligands.
abstract: As the serotonin transporter (SERT) is involved in several neurodegenerative and psychiatric disorders, radiopharmaceuticals to image the SERT by PET or SPECT would be very valuable in studying these diseases. For the development of imaging agents, we have synthesized novel derivatives of recently reported diphenylsulfide SERT ligands, in which the sulfur atom linking the two phenyl rings was replaced by an oxygen, sulfinyl, sulfonyl, amino or carbon group. Three of these exhibited good to high in vitro affinity (0.5 nM < K(i) < 11 nM) and selectivity for the SERT over the other monoamine transporters.
authors.affiliation: Université François Rabelais de Tours, INSERM U619, Laboratoire de Biophysique Médicale et Pharmaceutique, 31 avenue Monge, 37200 Tours, France.
authors.forename: Johnny
authors.initials: J
authors.lastname: Vercouillie
authors.forename: Sylvie
authors.initials: S
authors.lastname: Mavel
authors.forename: Laurent
authors.initials: L
authors.lastname: Galineau
authors.forename: Tiziana
authors.initials: T
authors.lastname: Ragusa
authors.forename: Robert
authors.initials: R
authors.lastname: Innis
authors.forename: Michael
authors.initials: M
authors.lastname: Kassiou
authors.forename: Sylvie
authors.initials: S
authors.lastname: Chalon
authors.forename: Frédéric
authors.initials: F
authors.lastname: Dollé
authors.forename: Jean-Claude
authors.initials: JC
authors.lastname: Besnard
authors.forename: Denis
authors.initials: D
authors.lastname: Guilloteau
authors.forename: Patrick
authors.initials: P
authors.lastname: Emond
mesh_terms: D020128:Inhibitory Concentration 50; D008024:Ligands; D015394:Molecular Structure; D012680:Sensitivity and Specificity; D050486:Serotonin Plasma Membrane Transport Proteins / Q000378:metabolism*; D013329:Structure-Activity Relationship; D013379:Substrate Specificity; D013440:Sulfides / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism*
chemical_list: D008024:Ligands; D050486:Serotonin Plasma Membrane Transport Proteins; D013440:Sulfides