Effects of U-37883A on intracellular Ca2+ -activated large-conductance K+ channels in pig proximal urethral myocytes.
Effects of U-37883A on intracellular Ca2+ -activated large-conductance K+ channels in pig proximal urethral myocytes.
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U-37883A 对猪近端尿道肌细胞内 Ca2 激活的大电导 K 通道的影响。
DOI：
10.1016/j.ejphar.2004.10.025
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发表时间：
2004
影响因子：
5
通讯作者：
Y. Ito
中科院分区：
文献类型：
--
作者：
N. Teramoto;M. Aishima;Hai‐Lei Zhu;T. Tomoda;T. Yunoki;F. Takahashi;A. Brading;Y. Ito
本文研究了血管ATP敏感性钾通道（KATP channel）阻断剂U-37883 A（4-morpholinecarboximidine-N-1-adamantyl-N′-hexacyclyl-hydrochloride）对猪尿道肌细胞内大电导Ca ~（2+）敏感性钾通道的抑制作用。BKC通道; 225 pS K+通道）。猪尿道平滑肌中的BKCa通道显示细胞外伊比利亚毒素（300 nM）敏感性和电压依赖性。Western blot检测细胞膜组分中BKCa通道蛋白α亚基的表达。应用U-37883 A（≥10 μM）以浓度依赖性方式降低BKC通道的活性，不仅通过降低平均开放时间，还通过延长平均关闭时间。这些结果表明，U-37883 A影响血管KATP通道以外的通道，并证明它如何抑制尿道平滑肌中的BKC通道的活性。
Kinetic studies of U-37883A (4-morpholinecarboximidine-N-1-adamantyl-N′-cyclohexyl-hydrochloride), a vascular ATP-sensitive K+channel (KATPchannel) blocker, were performed on pig urethral myocytes to investigate inhibitory effects on large-conductance intracellular Ca2+-sensitive K+channels (i.e., BKCachannels; 225 pS K+channels) by use of single-channel recordings (outside-out and inside-out configuration). BKCachannels in pig urethral smooth muscles showed extracellular iberiotoxin (300 nM) sensitivity and voltage dependency. The α subunit of BKCachannel proteins was detected in the membrane fraction by use of Western blot technique. Application of U-37883A (≥10 μM) reduced the activity of BKCachannels in a concentration-dependent manner, not only by decreasing mean openlife time but also by prolonging the mean closed time. These results shows that U-37883A affects channels other than the vascular KATPchannel, and demonstrates how it inhibits the activities of BKCachannels in urethral smooth muscles.
U-37883A 有效抑制大鼠纹状体神经元上多巴胺调节的 K 通道。
影响因子：
5
作者：
Lin,YJ;Chen,X;Freedman,JE
通讯作者：
Freedman,JE
影响因子：
3.4
作者：
SIGWORTH, FJ;SINE, SM
通讯作者：
SINE, SM