NS-1619 ACTIVATES BKCA CHANNEL ACTIVITY IN RAT CORTICAL-NEURONS

被引:34
作者
LEE, K [1 ]
ROWE, ICM [1 ]
ASHFORD, MLJ [1 ]
机构
[1] UNIV CAMBRIDGE,DEPT PHARMACOL,CAMBRIDGE CB2 1QJ,ENGLAND
基金
英国惠康基金;
关键词
NS; 1619; BKCA CHANNEL; NIFLUMIC ACID; MOTOR CORTEX;
D O I
10.1016/0014-2999(95)00251-F
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Single channel recordings of large conductance Ca2+-activated K+ (BKCa) channels were made from neurones isolated from rat motor cortex. Application of levcromakalim, pinacidil or diazoxide had no effect on BKCa channel activity in excised patches. In contrast, NS 1619 (1-(2'-hydroxy-5'-trifluoromethylphenyl)-5-trifluoromethyl-2(3H)benzimidazalone) induced concentration-dependent activation of BKCa channels with a calculated EC(50) of 32 mu M. The NS 1619-induced activity was dependent on the presence of free Ca2+ at the intracellular surface, but was not associated with a change in channel voltage sensitivity. Niflumic acid had no effect on BKCa activity per se but prevented NS 1619-mediated activation.
引用
收藏
页码:215 / 219
页数:5
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