Activation of rat recombinant α1β2γ2S GABAA receptor by the insecticide ivermectin
Activation of rat recombinant α1β2γ2S GABAA receptor by the insecticide ivermectin
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DOI：
10.1016/s0014-2999(00)00164-3
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发表时间：
2000-04-14
影响因子：
5
通讯作者：
Dudel, J
中科院分区：
文献类型：
--
作者：
Adelsberger, H;Lepier, A;Dudel, J
本文研究了伊维菌素对人胚肾（HEK）293细胞表达的大鼠重组α（1）β（2）γ（2s）γ-氨基丁酸（GABA）能氯离子通道的激活作用。通道的最大激活发生在GABA浓度为10 mM或20 μ M伊维菌素的情况下，这两种浓度都实现了大约相同的电流幅度。在这些饱和浓度下，电流在1 ms内随GABA上升至最大值，而伊维菌素的上升时间约为500倍。与GABA激活相反，伊维菌素在激动剂存在下未观察到脱敏。对于两种激动剂，检测到两种不同的开放状态。在同时应用GABA和伊维菌素时，电流幅度和动力学由在引发较高开放概率的浓度中应用的激动剂确定。它的结论是，GABA和伊维菌素激活通道独立导致不同的动力学特性。(C)2000 Elsevier Science B. V.保留所有权利。
In the present study, the activation of rat recombinant alpha(1)beta(2)gamma(2s) gamma-aminobutyric acid (GABA)-ergic Cl- channel expressed in human embryonic kidney (HEK) 293 cells by ivermectin was investigated. Maximal activation of the channel occurred with GABA concentrations of 10 mM or 20 mu M ivermectin both achieving about the same current amplitudes. With those saturating concentrations, the currents rose with GABA within 1 ms to the maximal values, whereas the rise time for ivermectin was about 500 times longer. In contrast to activation with GABA, no desensitisation in the presence of the agonist was observed with ivermectin. With both agonists, two different open states were detected. On simultaneous application of GABA and ivermectin the current amplitudes and the kinetics were determined by the agonist applied in the concentration eliciting the higher open probability. It is concluded that GABA and ivermectin activated the channel independently resulting in different kinetic properties. (C) 2000 Elsevier Science B.V. All rights reserved.