Open AccessNovel and High Affinity Fluorescent Ligands for the Serotonin Transporter Based on (S)-Citalopram
Author(s) -
Vivek Kumar,
Troels Rahbek-Clemmensen,
Christian B. Billesbølle,
Trine N. Jørgensen,
Ulrik Gether,
Amy Hauck Newman
Publication year - 2014
Publication title -
acs medicinal chemistry letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.065
H-Index - 66
ISSN - 1948-5875
DOI - 10.1021/ml5000806
Subject(s) - citalopram , serotonin transporter , norepinephrine transporter , serotonin , transporter , chemistry , dopamine transporter , transfection , rhodamine , biophysics , biochemistry , fluorescence , biology , receptor , gene , physics , quantum mechanics
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.