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

Vivek Kumar; Troels Rahbek-Clemmensen; Christian B Billesbølle; Trine Nygaard Jorgensen; Ulrik Gether; Amy Hauck Newman

doi:10.1021/ml5000806

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

Vivek Kumar, Troels Rahbek-Clemmensen, Christian B Billesbølle, Trine Nygaard Jorgensen, Ulrik Gether, Amy Hauck Newman

Neuropharm and Genetics

12 Citationer (Scopus)

Abstract

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.

Originalsprog	Engelsk
Tidsskrift	A C S Medicinal Chemistry Letters
Vol/bind	5
Udgave nummer	6
Sider (fra-til)	696-9
Antal sider	4
ISSN	1948-5875
DOI	https://doi.org/10.1021/ml5000806
Status	Udgivet - 12 jun. 2014

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10.1021/ml5000806

Citationsformater

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

abstract = "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.",

author = "Vivek Kumar and Troels Rahbek-Clemmensen and Billesb{\o}lle, {Christian B} and Jorgensen, {Trine Nygaard} and Ulrik Gether and Newman, {Amy Hauck}",

year = "2014",

month = jun,

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doi = "10.1021/ml5000806",

language = "English",

volume = "5",

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journal = "ACS Medicinal Chemistry Letters",

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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 - ACS Medicinal Chemistry Letters

JF - ACS Medicinal Chemistry Letters

IS - 6

ER -

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

Abstract

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