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Synthesis and in vitro evaluation of fluorinated diphenyloxide derivatives and sulfur analogs as serotonin transporter ligands.
- 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.)
- Subjects :
- Binding, Competitive
Cell Line, Tumor
Dopamine Plasma Membrane Transport Proteins metabolism
Halogenation
Humans
Ligands
Norepinephrine Plasma Membrane Transport Proteins metabolism
Phenyl Ethers chemical synthesis
Sulfides chemical synthesis
Sulfides chemistry
Sulfides pharmacology
Phenyl Ethers chemistry
Phenyl Ethers pharmacology
Serotonin Plasma Membrane Transport Proteins metabolism
Subjects
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