Cannell M B, Soeller C
Department of Pharmacology and Clinical Pharmacology, St. George's Hospital Medical School, London, England.
Biophys J. 1997 Jul;73(1):112-22. doi: 10.1016/S0006-3495(97)78052-4.
Computer simulations were used to examine the response of ryanodine receptors (RyRs) to the sarcolemmal calcium influx via L-type calcium channels (DHPRs). The effects of ryanodine receptor organization, diad geometry, DHPR single-channel current, and DHPR gating were examined. In agreement with experimental findings, the simulations showed that RyRs can respond rapidly (approximately 0.4 ms) to calcium influx via DHPRs. The responsiveness of the RyR depends on the geometrical arrangement between the RyRs and the DHPR in the diad, with wider diads being generally less responsive. When the DHPR single-channel current is small (approximately 25 fA), the organization of RyRs into small clusters results in an improved responsiveness. With experimentally observed DHPR mean open and closed times (0.17 ms and 4 ms, respectively) it is the first opening of the DHPR that is most likely to activate the RyR. A measure of the efficiency (Q) by which DHPR gating evokes sarcoplasmic reticulum release is defined. Q is at maximum for tau approximately 0.3 ms, and we interpret this finding in terms of the "tuning" of DHPR gating to RyR response. If certain cardiac myopathies are associated with a mismatch in the "tuning," then modification of DHPR gating with drugs to "retune" calcium-induced calcium release should be possible.
利用计算机模拟来研究兰尼碱受体(RyRs)对经由L型钙通道(二氢吡啶受体,DHPRs)的肌膜钙内流的反应。研究了兰尼碱受体的组织、二联体几何结构、DHPR单通道电流和DHPR门控的影响。与实验结果一致,模拟显示RyRs可对经由DHPRs的钙内流迅速做出反应(约0.4毫秒)。RyR的反应性取决于二联体中RyRs与DHPR之间的几何排列,一般来说,更宽的二联体反应性较低。当DHPR单通道电流较小时(约25飞安),RyRs组织成小簇会导致反应性提高。根据实验观察到的DHPR平均开放和关闭时间(分别为0.17毫秒和4毫秒),最有可能激活RyR的是DHPR的首次开放。定义了一种衡量DHPR门控引发肌浆网释放效率(Q)的指标。当时间常数(tau)约为0.3毫秒时,Q最大,我们根据DHPR门控对RyR反应的“调谐”来解释这一发现。如果某些心肌病与这种“调谐”不匹配有关,那么用药物改变DHPR门控以“重新调谐”钙诱导的钙释放应该是可行的。