Zeiske W, Wills N K, Van Driessche W
Biochim Biophys Acta. 1982 May 21;688(1):201-10. doi: 10.1016/0005-2736(82)90595-8.
(1) The effects of the Na+-channel blocker, amiloride, on the short-circuit current carried by Na+ was studied with fluctuation analysis, in rabbit descending colon epithelium. (2) In the presence of mucosal amiloride, the power spectrum of the Na+-current noise showed a Lorentzian component. When the Na+ current was reduced by increasing the blocker concentrations, the Lorentzian plateau decreased and corner frequency increased. Macroscopic short-circuit current and current-noise data are evidence for a two-state mechanism of the blocker interaction with the Na+ channel. (3) On- and off-rate constants for the blocker-receptor reaction, single-channel currents and Na+-channel density were calculated at room temperature and at 37 degrees C. Also, the activation energy for the amiloride-receptor reaction was estimated. The microscopic parameters obtained for the Na+ channel in the colon were similar to those found for Na+ channels in other tight epithelia.
(1)采用波动分析方法,在兔降结肠上皮中研究了钠通道阻滞剂氨氯地平对钠所携带的短路电流的影响。(2)在黏膜存在氨氯地平的情况下,钠电流噪声的功率谱显示出一个洛伦兹分量。当通过增加阻滞剂浓度降低钠电流时,洛伦兹平台降低,转折频率增加。宏观短路电流和电流噪声数据证明了阻滞剂与钠通道相互作用的双态机制。(3)在室温及37℃下计算了阻滞剂 - 受体反应的结合和解离速率常数、单通道电流和钠通道密度。此外,还估算了氨氯地平 - 受体反应的活化能。在结肠中获得的钠通道微观参数与在其他紧密上皮中发现的钠通道微观参数相似。