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[阿米啶和他克林对蜗牛神经元胆碱能受体活性及可塑性的调节:现象学与机制]

[The amiridin and tacrine modulation of the cholinoreceptor activity and plasticity of snail neurons: the phenomenology and mechanisms].

作者信息

Burov Iu V, Drozdova E I, Pivovarov A S, Robakidze T N

出版信息

Zh Vyssh Nerv Deiat Im I P Pavlova. 1993 Nov-Dec;43(6):1202-9.

PMID:8135063
Abstract

The effects of amiridine and tacrine on the membrane potential, activity and plasticity of cholinoreceptors have been studied using the recording of intracellular and transmembrane currents in identified neurons of Helix lucorum. Amiridine and tacrine (1-100 mcM) have no noticeable effects on the membrane potential of the cells. Both compounds modulate the activity of cholinoreceptors to judge from their influence on the inward current induced by the local acetylcholine (ACh) application: they increase the duration of the current with a two-phase effect on the amplitude (a short-latent intensification with a following decrease). Amiridine and tacrine intensify ACh current extinction induced by repeated ACh application to the soma. Acetylcholinesterase inhibitor physostigmine has a similar modulating effect on ACh current and its extinction. It impedes the modulating effects of amiridine and tacrine. Amiridine and physostigmine directly affect cholinoreceptors and ion channels controlled by them changing in a similar way the current-voltage curves of ACh-current and approximating it to the equilibrium potential of chloride ions. Modulating effects of amiridine, tacrine and physostigmine on the activity and plasticity of cholinoreceptors may be supposed to be caused by their direct membrane-cytoplasmic action.

摘要

利用对福寿螺特定神经元内电流和跨膜电流的记录,研究了阿米啶和他克林对胆碱能受体膜电位、活性和可塑性的影响。阿米啶和他克林(1 - 100微摩尔)对细胞的膜电位没有明显影响。从它们对局部应用乙酰胆碱(ACh)所诱导的内向电流的影响来判断,这两种化合物均能调节胆碱能受体的活性:它们增加电流持续时间,对电流幅度有双相作用(短暂潜伏期增强后下降)。阿米啶和他克林增强了向胞体重复应用ACh所诱导的ACh电流消退。乙酰胆碱酯酶抑制剂毒扁豆碱对ACh电流及其消退具有类似的调节作用。它阻碍了阿米啶和他克林的调节作用。阿米啶和毒扁豆碱直接影响胆碱能受体及其控制的离子通道,以类似方式改变ACh电流的电流 - 电压曲线,并使其接近氯离子的平衡电位。阿米啶、他克林和毒扁豆碱对胆碱能受体活性和可塑性的调节作用可能是由它们直接的膜 - 细胞质作用引起的。

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