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ACS Med Chem Lett. 2014 Mar 27;5(6):696-9. doi: 10.1021/ml5000806. eCollection 2014.

Novel and high affinity fluorescent ligands for the serotonin transporter based on (s)-citalopram.

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  • 1Medicinal Chemistry Section, Molecular Targets and Medications Discovery Branch, National Institute on Drug Abuse-Intramural Research Program, National Institutes of Health , 333 Cassell Drive, Baltimore, Maryland 21224, United States.
  • 2Molecular Neuropharmacology Laboratory and Center for Pharmacogenomics, Department of Neuroscience and Pharmacology, The Faculty of Health and Medical Sciences, University of Copenhagen , DK-2200 Copenhagen N, Denmark.


Novel rhodamine-labeled ligands, based on (S)-citalopram, were synthesized and evaluated for uptake inhibition at the human serotonin, dopamine, and norepinephrine transporters (hSERT, hDAT, and hNET, respectively) and for binding at SERT, in transiently transfected COS7 cells. Compound 14 demonstrated high affinity binding and selectivity for SERT (K i = 3 nM). Visualization of SERT, using confocal laser scanning microscopy, validated compound 14 as a novel tool for studying SERT expression and distribution in living cells.


Fluorescent ligand; SERT; citalopram; rhodamine

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