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SKF38393抑制大鼠DRG分离神经元GABA-激活电流

李琴, 王钦文, 李之望

同济医科大学实验医学研究中心；武汉市职工医学院生理教研室

摘要

在大鼠新鲜分离DRG神经元标本上应用全细胞膜片箝记录，观察了多巴胺D1受体的选择性激动剂（±）SKF38393HCI对GABA-激活电流的作用。大部分受检细胞（60／70）对GABA敏感，10－6－10－3mol／LGABA可引起呈剂量依赖性的明显去敏感作用的内向电流。在这60个细胞中，预加SKF38393可引起三类膜反应如：（1）外向电流（7／60）；（2）内向电流（5／60）和（3）无反应（48／60）。与GANA激活的内向电流相比，SKF38393激活电流幅值较小，无明显去敏感现象。预加SKF3839330s对GABA-激活电流幅值的影响如下：产生抑制作用的为53／60，增强的为1／60，无明显作用的为6／60。在浓度10-7至10－4mol／L范围SKF38393对10－4mol／L的GANA-激活电流的抑制作用依赖于SKF38393的浓度。通过应用二次膜片箝（repatch）技术在同一细胞（n＝2）以及不同细胞组间（n＝14）进行对比，结果表明：细胞内加蛋白激酶抑制剂H－7后，SKF38393对GANA的抑制作用完全消除，看来SKF38393对GABA-激活电流的抑制作用可能是由于SKF38393使CABA受体通道复合体胞内磷酸化所致。

关键词： 背根神经节; 全细胞膜片箝记录; 多巴胺D_1-受体激动剂SKF38393; γ-氨基丁酸; 抑制作用

Cui Hong

First Clinical Institute，China Medical University. Shenyang 110001,Liaoning, China

Abstract

Experiments were Performed on neurons freshly isolated from rat DRG using wholecell patch-clamp techniqUes. The majority of the neurons examined were sensitive to GABA (60/70) in the concentration range from 10-6 to 10-3 mol/L, showing obvious desensihzation. In the 60 GABA-sensitive cells, responses induced by selective agonist Of dopamine D1 receptor Sin8393 [ (±) SKF38393HCL] manifested three types: (1)outward current (7/60); (2) inward current (5/60) and (3) no detectable response (48/60). As compared with GABA-activated current, the amplitude of SKF38393activated current are smaller and showed no apparent desensitization. When the neurons were treated with SKF38393 prior to application of GABA for 30 s, the GABA-activated current in majority of the cells (53/60) was inhibited, while the remaining six showed no effect. The effect of Sin8393 was dose dependent.

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引用本文：

李琴, 王钦文, 李之望. SKF38393抑制大鼠DRG分离神经元GABA-激活电流[J]. 生理学报 1998; 50 (3): .

Cui Hong. . Acta Physiol Sin 1998; 50 (3): (in Chinese with English abstract).