2 research outputs found
Novel and high affinity fluorescent ligands for the serotonin transporter based on (s)-citalopram
[Image: see text] 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
Novel and High Affinity Fluorescent Ligands for the Serotonin Transporter Based on (<i>S</i>)‑Citalopram
Novel
rhodamine-labeled ligands, based on (<i>S</i>)-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 <b>14</b> demonstrated high affinity binding
and selectivity for SERT (<i>K</i><sub>i</sub> = 3 nM).
Visualization of SERT, using confocal laser scanning microscopy, validated
compound <b>14</b> as a novel tool for studying SERT expression
and distribution in living cells