title: Novel and high affinity fluorescent ligands for the serotonin transporter based on (s)-citalopram.
abstract: 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.
authors.affiliation: Medicinal 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.
authors.forename: Vivek
authors.initials: V
authors.lastname: Kumar
authors.affiliation: Molecular 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.
authors.forename: Troels
authors.initials: T
authors.lastname: Rahbek-Clemmensen
authors.affiliation: Molecular 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.
authors.forename: Christian B
authors.initials: CB
authors.lastname: Billesbølle
authors.affiliation: Molecular 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.
authors.forename: Trine Nygaard
authors.initials: TN
authors.lastname: Jorgensen
authors.affiliation: Molecular 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.
authors.forename: Ulrik
authors.initials: U
authors.lastname: Gether
authors.affiliation: Medicinal 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.
authors.forename: Amy Hauck
authors.initials: AH
authors.lastname: Newman
keywords: Fluorescent ligand; SERT; citalopram; rhodamine