Abstract
In order to predict affinity of new diphenylsulfides for the serotonin transporter (SERT), a molecular modeling model was used to compare potential binding affinity of new compounds with known potent ligands. The aim of this study is to identify a suitable PET radioligand for imaging the SERT, new derivatives, and their precursors for a C-11 or F-18 radiolabeling, were synthesized. Two fluorinated derivatives displayed good in vitro affinity for the SERT (K(i)=14.3+/-1 and 10.1+/-2.7 nM) and good selectivity toward the other monoamine transporters as predicted by the docking study.
Publication types
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Evaluation Study
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Research Support, Non-U.S. Gov't
MeSH terms
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Algorithms*
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Benzylamines* / chemical synthesis
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Carbon Radioisotopes / chemistry
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Cell Line
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Diagnostic Imaging / methods*
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Fluorine Radioisotopes / chemistry*
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Humans
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Kidney / cytology
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Kidney / embryology
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Kidney / pathology
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Ligands
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Membrane Transport Proteins / chemistry
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Membrane Transport Proteins / metabolism*
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Positron-Emission Tomography / methods*
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Reproducibility of Results
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Sensitivity and Specificity
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Serotonin Plasma Membrane Transport Proteins / chemistry
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Serotonin Plasma Membrane Transport Proteins / metabolism*
Substances
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Benzylamines
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Carbon Radioisotopes
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Fluorine Radioisotopes
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Ligands
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Membrane Transport Proteins
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N,N-dimethyl-2-(2-amino-4-methylphenylthio)benzylamine
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Serotonin Plasma Membrane Transport Proteins