Activation of human IK and SK Ca2+-activated K+ channels by NS309 (6,7-dichloro-1H-indole-2,3-dione 3-oxime)

被引:158
作者
Strobæk, D [1 ]
Teuber, L [1 ]
Jorgensen, TD [1 ]
Ahring, PK [1 ]
Kjær, K [1 ]
Hansen, RS [1 ]
Olesen, SP [1 ]
Christophersen, P [1 ]
Skaaning-Jensen, B [1 ]
机构
[1] NeuroSearch AS, DK-2750 Ballerup, Denmark
来源
BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES | 2004年 / 1665卷 / 1-2期
关键词
Ca2+ -activated K+ channel; hIK; hSK; 1-EbIO; DC-EBIO; apamin; clotrimazole; whole-cell; HEK293;
D O I
10.1016/j.bbamem.2004.07.006
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
We have identified and characterized the compound NS309 (6,7-dichloro-1H-indole-2,3-dione 3-oxime) as a potent activator of human Ca2+-activated K+ channels of SK and IK types, whereas it is devoid of effect on BK type channels. IK- and SK-channels have previously been reported to be activated by the benzimidazolinone, 1-EBIO and more potently by its dichloronated-analogue, DC-EBIO. NS309 is at least 1000 times more potent than 1-EBIO and at least 30 times more potent than DC-EBIO when the compounds are compared on the same cell. (C) 2004 Elsevier B.V. All rights reserved.
引用
收藏
页码:1 / 5
页数:5
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