Illuminating the norepinephrine transporter: fluorescent probes based on nisoxetine and talopram

文献情報

出版日 2021-06-09

DOI 10.1039/D1MD00072A

インパクトファクター 0

著者

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

原文を見る

要旨

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.

掲載誌

RSC Medicinal Chemistry

CiteScore: 0

自己引用率: 0%

年間論文数: 0

Illuminating the norepinephrine transporter: fluorescent probes based on nisoxetine and talopram

文献情報

おすすめジャーナル

関連文献

Interaction of water with oligo(ethylene glycol) terminated monolayers: wetting versus hydration

The structural α-relaxation times of prilocaine confined in 1 nm pores of molecular sieves: quantitative explanation by the coupling model

Impact of t-butyl substitution in a rubrene emitter for solid state NIR-to-visible photon upconversion

Hierarchical phenomena in multicomponent liquids: simulation methods, analysis, chemistry

Gas phase reactions of iodide and bromide anions with ozone: evidence for stepwise and reversible reactions‡

Unusual intrinsic thermoluminescence in LiMgPO4:Er

Yields of primary species in the low-linear energy transfer radiolysis of water in the temperature range of 25–700 °C

Front cover

Penning spectroscopy and structure of acetylene oligomers in He nanodroplets

Gate voltage impact on charge mobility in end-on stacked conjugated oligomers

こちらもおすすめ

2-ヒドロキシ-5-ニトロベンジンブロモイドの代替品はありますか？

N-(2-ブロモフェニル)-1-チロール-3-オキソ-3-(ピペリジニル)プロペン-2-イル)ベンゼンアミドを取り扱う際の実験室安全事項は何ですか？

1,3プロパンジオール,2-[2-(2アミノ-6クロロ-9Hピリミジン-9-イル)エチル-1,1,2,2-D4]-2,3-ジアセタートの市場動向や研究トレンドはどうですか？

安息香の代替品はありますか？

Succinimidyl-alanyl-phenylalanyl-prolyl-phenylalanine 4-nitroanilide はどの業界で使用されていますか？

メチル6-アミノ-5-クロロピリジン-2-カーボイル酸について、適用される法規ガイドラインは何ですか？

エチル4-(シクロ Pentagonyl)アミノ-2-メチル硫化基ピリミジン-5-カルボキシレートを取り扱う際の実験室安全事項は何ですか？

（S）-3-ベンZYルピペリジン塩酸塩とは何ですか？

3,5-二甲基金剛胺の主な用途は何ですか？

ビス(4-メチル-2-ペンチル)フェニルカルボン酸エステルの代替品はありますか？

掲載誌

RSC Medicinal Chemistry

おすすめ化合物

1-[3-(4-Morpholinylsulfonyl)phenyl]methanamine

6-Bromo-2,3-dihydro-4H-thiochromen-4-one

4-Methyl-3-phenyl-2-piperazinone

Methyl 4-({[(2-methyl-2-propanyl)oxy]carbonyl}amino)bicyclo[2.2.2]octane-1-carboxylate

1H-1,2,4-triazol-5-ylmethanol

おすすめサプライヤー