4-Benzyl-1-(tert-butoxycarbonyl)piperidine-4-carboxylic acid
CAS Number:
170838-87-6
Molecular Formula:
C18H25NO4
Illuminating the norepinephrine transporter: fluorescent probes based on nisoxetine and talopram
Literature Information
Publication Date
2021-06-09
DOI
10.1039/D1MD00072A
Impact Factor
0
Authors
Gisela Andrea Camacho-Hernandez, Deborah Rudin, Therese C. Ku, Daryl A. Guthrie, Valentina Straniero, Ermanno Valoti, Gerhard J. Schütz, Harald H. Sitte, Amy Hauck Newman
View Original
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 probe 6 demonstrated 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, compound 6 was shown to stain both NET and SERT, but not DAT, at low nanomolar concentrations, in transporter-expressing cells.
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Source Journal
Recommended Compounds
3-Chloro-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2-pyridinamine
CAS Number:
1032758-99-8
Molecular Formula:
C11H16BClN2O2
![tert-Butyl N-[(2-chloropyridin-4-yl)methyl]carbamate structure](https://static.chemtradehub.com/structs/916/916210-27-0-9f95.webp "tert-Butyl N-[(2-chloropyridin-4-yl)methyl]carbamate structure")
tert-Butyl N-[(2-chloropyridin-4-yl)methyl]carbamate
CAS Number:
916210-27-0
Molecular Formula:
C11H15ClN2O2
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