MECHANISM OF ACTION OF A K+ CHANNEL ACTIVATOR BRL-38227 ON ATP-SENSITIVE K+ CHANNELS IN MOUSE SKELETAL-MUSCLE FIBERS
MECHANISM OF ACTION OF A K+ CHANNEL ACTIVATOR BRL-38227 ON ATP-SENSITIVE K+ CHANNELS IN MOUSE SKELETAL-MUSCLE FIBERS
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DOI：
10.1113/jphysiol.1994.sp020271
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发表时间：
1994-08-01
影响因子：
5.5
通讯作者：
HEAD, SI
中科院分区：
文献类型：
--
作者：
HUSSAIN, M;WAREHAM, AC;HEAD, SI
1. 研究了钾通道激活剂BRL 38227对C57BL/6J小鼠指屈肌解离的单纤维中ATP敏感钾通道(K（ATP)（+）通道）的影响。在细胞贴附斑块中，BRL 38227 （100 μ M）引起格列本脲敏感钾电流的激活。向内电流的线性斜率电导、向外电流的部分整流和格列本脲的灵敏度表明，K-ATP（+）通道是BRL 38227.3的作用位点。在切除的内外斑块细胞质侧缺乏ATP的情况下，BRL 38227引起K-ATP（+）通道的直接和镁依赖性激活。随着BRL 38227.4的连续应用，激活程度降低。BRL 38227在低(
1. Investigations were made into the effects of BRL 38227, a potassium channel activator, on ATP-sensitive potassium channels (K(ATP)(+)channels) in single fibres dissociated from the flexor digitorum brevis muscle of C57BL/6J mice.2. In cell-attached patches BRL 38227 (100 mu M) caused activation of a glibenclamide-sensitive potassium current. Linear slope conductance of the inward current, partial rectification of the outward current and glibenclamide sensitivity indicate that K-ATP(+) channels are the site of action of BRL 38227.3. In the absence of ATP at the cytoplasmic side of excised inside-out patches, BRL 38227 caused direct and magnesium-dependent activation of K-ATP(+) channels. The degree of activation diminished with successive applications of BRL 38227.4. BRL 38227 also caused activation of K-ATP(+) channels in the presence of low(