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Medchemcomm. 2019 Feb 26;10(4):513-516. doi: 10.1039/c8md00562a. eCollection 2019 Apr 1.
2
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Astemizole Derivatives as Fluorescent Probes for hERG Potassium Channel Imaging.作为用于人乙醚 - 去极化相关基因（hERG）钾通道成像的荧光探针的阿司咪唑衍生物。
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Cell. 2017 Apr 20;169(3):422-430.e10. doi: 10.1016/j.cell.2017.03.048.
2
Highly sensitive HPLC method for the determination of galantamine in human plasma and urine through derivatization with dansyl chloride using fluorescence detector.
Luminescence. 2017 Nov;32(7):1145-1149. doi: 10.1002/bio.3301. Epub 2017 Apr 21.
3
Astemizole Derivatives as Fluorescent Probes for hERG Potassium Channel Imaging.作为用于人乙醚 - 去极化相关基因（hERG）钾通道成像的荧光探针的阿司咪唑衍生物。
ACS Med Chem Lett. 2016 Jan 20;7(3):245-9. doi: 10.1021/acsmedchemlett.5b00360. eCollection 2016 Mar 10.
4
Environment-Sensitive Fluorescent Probe for the Human Ether-a-go-go-Related Gene Potassium Channel.用于人类醚-去极化相关基因钾通道的环境敏感型荧光探针。
Anal Chem. 2016 Feb 2;88(3):1511-5. doi: 10.1021/acs.analchem.5b04220. Epub 2016 Jan 8.
5
Evaluation of DNA Binding, Radicals Scavenging and Antimicrobial Studies of Newly Synthesized N-Substituted Naphthalimides: Spectroscopic and Molecular Docking Investigations.新合成的N-取代萘二甲酰亚胺的DNA结合、自由基清除及抗菌研究评估：光谱和分子对接研究
J Fluoresc. 2015 Nov;25(6):1905-20. doi: 10.1007/s10895-015-1683-1. Epub 2015 Oct 13.
6
Cell-trappable fluorescent probes for endogenous hydrogen sulfide signaling and imaging H2O2-dependent H2S production.用于内源性硫化氢信号转导的细胞捕获型荧光探针及检测 H2O2 依赖性 H2S 产生的荧光探针。
Proc Natl Acad Sci U S A. 2013 Apr 30;110(18):7131-5. doi: 10.1073/pnas.1302193110. Epub 2013 Apr 15.
7
Fluorescent probes for sensing and imaging biological hydrogen sulfide.用于检测和成像生物硫化氢的荧光探针。
Curr Opin Chem Biol. 2012 Dec;16(5-6):595-601. doi: 10.1016/j.cbpa.2012.07.014. Epub 2012 Aug 23.
8
Pharmacophore modeling for hERG channel facilitation.配体药效团模型构建用于 hERG 通道促进。
Biochem Biophys Res Commun. 2012 Feb 3;418(1):161-6. doi: 10.1016/j.bbrc.2011.12.153. Epub 2012 Jan 8.
9
Novel roles for hERG K(+) channels in cell proliferation and apoptosis.hERG K(+) 通道在细胞增殖和凋亡中的新作用。
Cell Death Dis. 2011 Aug 18;2(8):e193. doi: 10.1038/cddis.2011.77.
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Fluorescent and luminescent probes for detection of reactive oxygen and nitrogen species.用于检测活性氧和氮物种的荧光和发光探针。
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用于成像人乙醚-去极化激活的钾离子通道（hERG钾通道）的基于阿司咪唑的开启型荧光探针。

Astemizole-based turn-on fluorescent probes for imaging hERG potassium channel.

作者信息

Zhang Xiaomeng, Liu Tingting, Wang Beilei, Gao Yuqi, Liu Pan, Li Minyong, Du Lupei

机构信息

Department of Medicinal Chemistry , Key Laboratory of Chemical Biology (MOE) , School of Pharmacy , Shandong University , Jinan , Shandong 250012 , China . Email:

出版信息

Medchemcomm. 2019 Feb 26;10(4):513-516. doi: 10.1039/c8md00562a. eCollection 2019 Apr 1.

DOI:10.1039/c8md00562a
PMID:31057730
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6482408/
Abstract

Based on the scaffold of astemizole, three novel turn-on fluorescent probes (-) for human ether-a-go-go-related gene (hERG) potassium channel were developed herein. These probes have reasonable fluorescence properties, acceptable cell toxicity, and potent inhibitory activity, all of which contribute to cell imaging at the nanomolar level. Overall, these probes have the potential for setting up a screening system for hERG channels.

摘要

基于阿司咪唑的骨架，本文开发了三种新型的用于人醚 - 去极化相关基因（hERG）钾通道的开启型荧光探针（-）。这些探针具有合理的荧光特性、可接受的细胞毒性和有效的抑制活性，所有这些都有助于在纳摩尔水平上进行细胞成像。总体而言，这些探针具有建立hERG通道筛选系统的潜力。