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首页> 外文期刊>Life sciences >Characterization of chromanol 293B-induced block of the delayed-rectifier K(+) current in heart-derived H9c2 cells.
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Characterization of chromanol 293B-induced block of the delayed-rectifier K(+) current in heart-derived H9c2 cells.

机译：苯二甲酚293B诱导的心脏源性H9c2细胞中延迟整流器K（+）电流阻滞的表征。

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摘要

The effects of chromanol 293B on ion currents in rat embryonic heart-derived H9c2 cells were investigated in this study. Chromanol 293B suppressed the amplitude of delayed rectified K(+) current (I(K)) in a concentration-dependent manner. The IC(50) value for chromanol 293B-induced inhibition of I(K) was 8 muM. The I(K) present in these cells, the electrical properties of which resembled those for the Kv2.1-related K(+) current, was sensitive to inhibition by quinidine or dendrotoxin, yet not by pandinotoxin-Kalpha, E-4031 or apamin. Chromanol 293B reduced the activation time constant of I(K) and the effective gating charge of this channel. However, little or no modification in the steady-state inactivation of I(K) in response to long-lasting conditioning pulses could be demonstrated in the presence of chromanol 293B. These results clearly demonstrate that chromanol 293B can effectively interact with the K(+) channel functionally expressed in H9c2 myoblasts. The chromanol 293B-induced inhibition of these channels could primarily be attributed to open channel block.
机译：本研究研究了苯并二氢苯并三氢邻苯二酚293B对大鼠胚胎心脏H9c2细胞离子电流的影响。铬醇293B以浓度依赖的方式抑制了延迟整流K（+）电流（I（K））的幅度。苯并三酚293B诱导的I（K）抑制的IC（50）值为8μM。这些细胞中存在的I（K）的电特性类似于Kv2.1相关K（+）电流的I（K）对奎尼丁或树突毒素的抑制作用敏感，但对pandinotoxin-Kalpha，E-4031或阿帕明。 Chromanol 293B降低了I（K）的激活时间常数和该通道的有效门控电荷。但是，在存在色酚293B的情况下，可以证明响应于持久的调节脉冲，I（K）的稳态失活几乎没有改变。这些结果清楚地表明，苯并二氢吡喃酚293B可以与H9c2成肌细胞中功能性表达的K（+）通道有效相互作用。苯并二氢苯并二氢吡喃并293B对这些通道的抑制作用主要归因于开放通道阻滞。

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