Department of Cellular and Physiological Sciences, University of British Columbia, 2350 Health Sciences Mall, Vancouver, BC, Canada V6T 1Z3.
J Physiol. 2010 Aug 15;588(Pt 16):3011-30. doi: 10.1113/jphysiol.2010.191544. Epub 2010 Jun 25.
External H+ and Ni2+ ions inhibit Kv1.5 channels by increasing current decay during a depolarizing pulse and reducing the maximal conductance. Although the former may be attributed to an enhancement of slow inactivation occurring from the open state, the latter cannot. Instead, we propose that the loss of conductance is due to the induction, by H+ or Ni2+, of a resting inactivation process. To assess whether the two inactivation processes are mechanistically related, we examined the time courses for the onset of and recovery from H+- or Ni2+-enhanced slow inactivation and resting inactivation. Compared to the time course of H+- or Ni2+-enhanced slow inactivation at +50 mV, the onset of resting inactivation induced at 80 mV with either ion involves a relatively slower process. Recovery from slow inactivation under control conditions was bi-exponential, indicative of at least two inactivated states. Recovery following H+- or Ni2+-enhanced slow inactivation or resting inactivation had time constants similar to those for recovery from control slow inactivation, although H+ and Ni2+ biased inactivation towards states from which recovery was fast and slow, respectively. The shared time constants suggest that the H+- and Ni2+-enhanced slow inactivated and induced resting inactivated states are similar to those visited during control slow inactivation at pH 7.4. We conclude that in Kv1.5 H+ and Ni2+ differentially enhance a slow inactivation process that involves at least two inactivated states and that resting inactivation is probably a close variant of slow inactivation.
外部 H+ 和 Ni2+ 离子通过增加去极化脉冲过程中的电流衰减并降低最大电导来抑制 Kv1.5 通道。虽然前者可能归因于从开放状态发生的缓慢失活的增强,但后者不能。相反,我们提出电导的损失是由于 H+或 Ni2+诱导的静息失活过程。为了评估这两种失活过程在机制上是否相关,我们研究了 H+或 Ni2+增强的缓慢失活和静息失活起始和恢复的时间过程。与 +50 mV 时 H+或 Ni2+增强的缓慢失活的时间过程相比,用任一离子在 80 mV 诱导的静息失活的起始涉及相对较慢的过程。在对照条件下,从缓慢失活中恢复是双指数的,表明至少存在两种失活状态。在 H+或 Ni2+增强的缓慢失活或静息失活后恢复的时间常数与对照缓慢失活后恢复的时间常数相似,尽管 H+和 Ni2+分别使失活偏向快速和慢速恢复的状态。共同的时间常数表明,H+和 Ni2+增强的缓慢失活和诱导的静息失活状态与在 pH 7.4 下进行对照缓慢失活时所经历的状态相似。我们得出结论,在 Kv1.5 中,H+和 Ni2+ 差异增强了至少涉及两种失活状态的缓慢失活过程,而静息失活可能是缓慢失活的密切变体。