Synthesis and in vitro evaluation of novel derivatives of diphenylsulfide as serotonin transporter ligands |
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| Authors: | Vercouillie Johnny Mavel Sylvie Galineau Laurent Ragusa Tiziana Innis Robert Kassiou Michael Chalon Sylvie Dollé Frédéric Besnard Jean-Claude Guilloteau Denis Emond Patrick |
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| Affiliation: | 1. Regional Centre of Advanced Technologies and Materials, Department of Inorganic Chemistry, Faculty of Science, Palacký University in Olomouc, 17. listopadu 12, CZ-771 46 Olomouc, Czech Republic;2. Department of Human Pharmacology and Toxicology, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences Brno, Palackého tř. 1/3, CZ-612 42 Brno, Czech Republic |
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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 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. |
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