Kass R S
J Pharmacol Exp Ther. 1982 Nov;223(2):446-56.
Nisoldipine is a new dihydropyridine derivative which is structurally related to the calcium current blocker nifedipine. In this paper, the effects of this new blocker are studied on Purkinje fiber plateau currents and are compared with the effects of D600 on the same currents. The results show that, like D600, at concentrations near 10 microM nisoldipine can completely block the slow inward current and contractile activation. As is the case for D600, at these concentrations, nisoldipine reduces the transient outward current. However, in contrast to D600 and other calcium current blockers, this new compound does not reduce the delayed rectifier. In addition, these experiments indicate that the block of slow inward current by nisoldipine is much less sensitive to membrane potential than is the case for the block by D600 of this current. These results show that nisoldipine is a more selective calcium current blocker than previously studied compounds and suggest that it may be useful both as an experimental and a therapeutic tool.
尼索地平是一种新的二氢吡啶衍生物，在结构上与钙电流阻滞剂硝苯地平相关。本文研究了这种新阻滞剂对浦肯野纤维平台电流的影响，并将其与D600对相同电流的影响进行了比较。结果表明，与D600一样，在浓度接近10微摩尔时，尼索地平可完全阻断缓慢内向电流和收缩激活。与D600的情况一样，在这些浓度下，尼索地平会降低瞬时外向电流。然而，与D600和其他钙电流阻滞剂不同的是，这种新化合物不会降低延迟整流电流。此外，这些实验表明，尼索地平对缓慢内向电流的阻断对膜电位的敏感性远低于D600对该电流的阻断。这些结果表明，尼索地平是一种比先前研究的化合物更具选择性的钙电流阻滞剂，并表明它可能作为一种实验工具和治疗工具都有用。
