Simulation of use-dependent uptake of ion channel blocking agents by excitable membranes.

Simulation of use-dependent uptake of ion channel blocking agents by excitable membranes.
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模拟可兴奋膜对离子通道阻断剂的使用依赖性吸收。

DOI:
10.1109/tbme.1985.325492
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发表时间:
1985
期刊:
IEEE transactions on bio-medical engineering
影响因子:
--
通讯作者:
Kerr,RB
Kerr,RB
中科院分区:
--
文献类型:
--
作者:
Starmer,CF;Kerr,RB

文献摘要

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由于观察到的通道阻断过程的使用和频率依赖性,离子通道阻断剂很难进行动力学表征。提出了一种离子通道阻断模型,该模型基于来自膜片钳研究的单通道观察和控制配体池和通道结合位点之间扩散路径的霍奇金-赫胥利型通道门。该模型有助于估计和模拟许多局部麻醉剂和抗心律失常药物的药效学特性。所得到的模型很容易在小型数字计算机上实现。
Ion channel blocking agents have been difficult to characterize kinetically due to the use-and frequency-dependent nature of the observed channel blockade process. A model of ion channel blockade is presented which is based on single channel observations derived from patch clamp studies and a Hodgkin-Huxley-type channel gate that controls the diffusion path between ligand pool and the channel binding site. This model facilitates estimation and simulation of the pharmacodynamic properties of many local anesthetics and antiarrhythmic agents. The resulting model is easily implemented on small digital computers.