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

TY - JOUR

T1 - Novel and high affinity fluorescent ligands for the serotonin transporter based on (s)-citalopram

AU - Kumar, Vivek

AU - Rahbek-Clemmensen, Troels

AU - Billesbølle, Christian B

AU - Jorgensen, Trine Nygaard

AU - Gether, Ulrik

AU - Newman, Amy Hauck

PY - 2014/6/12

Y1 - 2014/6/12

N2 - 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.

AB - 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.

U2 - 10.1021/ml5000806

DO - 10.1021/ml5000806

M3 - Journal article

C2 - 24944746

SN - 1948-5875

VL - 5

SP - 696

EP - 699

JO - A C S Medicinal Chemistry Letters

JF - A C S Medicinal Chemistry Letters

IS - 6

ER -