Illuminating the norepinephrine transporter: fluorescent probes based on nisoxetine and talopram
Articolo
Data di Pubblicazione:
2021
Citazione:
Illuminating the norepinephrine transporter: fluorescent probes based on nisoxetine and talopram / G.A. Camacho-Hernandez, A. Casiraghi, D. Rudin, D. Luethi, T.C. Ku, D.A. Guthrie, V. Straniero, E. Valoti, G.J. Schutz, H.H. Sitte, A.H. Newman. - In: RSC MEDICINAL CHEMISTRY. - ISSN 2632-8682. - 12:7(2021 Jul 01), pp. 1174-1186. [10.1039/d1md00072a]
Abstract:
The utilization of fluorescent ligands to study the monoamine transporters (MATs) has increased our knowledge of their function and distribution in live cell systems. In this study, we extend SAR for nisoxetine and talopram as parent compounds, to identify high affinity rhodamine-labeled fluorescent probes for the norepinephrine transporter (NET). Nisoxetine-based fluorescent probe6demonstrated high binding affinity (Ki= 43 nM) for NET and an overall selectivity compared to the other transporters for dopamine (DAT;Ki= 1540 nM) and serotonin (SERT;Ki= 785 nM) in competitive radioligand binding assays. Using confocal microscopy, compound6was shown to stain both NET and SERT, but not DAT, at low nanomolar concentrations, in transporter-expressing cells.
Tipologia IRIS:
01 - Articolo su periodico
Elenco autori:
G.A. Camacho-Hernandez, A. Casiraghi, D. Rudin, D. Luethi, T.C. Ku, D.A. Guthrie, V. Straniero, E. Valoti, G.J. Schutz, H.H. Sitte, A.H. Newman
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