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乙二胺类似物和γ-氨基丁酸对皮质和苍白球神经元作用的比较。

Comparison of the effects of ethylenediamine analogues and gamma-aminobutyric acid on cortical and pallidal neurones.

作者信息

Perkins M N, Stone T W

出版信息

Br J Pharmacol. 1982 Jan;75(1):93-9. doi: 10.1111/j.1476-5381.1982.tb08761.x.

Abstract

1 The actions of ethylenediamine (EDA) and structurally related compounds were investigated by microiontophoresis in Wistar rats. 2 EDA inhibited, via a bicuculline-sensitive mechanism, the spontaneous firing rate of all cortical and pallidal cells tested. 3 The results with the analogues suggest that two amine groups are required for this neuronal depressant action whereas a carboxyl grouping is not. N-substitution reduces the depressant effect. The length of the molecule is also critical, more than 3 methylene components seriously reducing its effectiveness. A rigid analogue of EDA, piperazine, was also active. In addition the apparent transport numbers of EDA and gamma-aminobutyric acid (GABA) were calculated, showing a close similarity between the two. 4 The results are discussed wih respect to the possibility that EDA may represent a new class of GABA-mimetics, or may indicate the existence of a novel diamine receptor mediating bicuculline-sensitive inhibition in the rat CNS.

摘要
  1. 通过微离子电泳法在Wistar大鼠中研究了乙二胺(EDA)及其结构相关化合物的作用。2. EDA通过一种荷包牡丹碱敏感机制,抑制了所有受试皮质和苍白球细胞的自发放电率。3. 类似物的结果表明,这种神经元抑制作用需要两个胺基,而羧基则不需要。N-取代会降低抑制作用。分子长度也很关键,超过3个亚甲基成分会严重降低其有效性。EDA的刚性类似物哌嗪也具有活性。此外,还计算了EDA和γ-氨基丁酸(GABA)的表观迁移数,结果表明两者非常相似。4. 讨论了这些结果,涉及EDA可能代表一类新的GABA模拟物,或者可能表明存在一种新型二胺受体介导大鼠中枢神经系统中荷包牡丹碱敏感抑制作用的可能性。

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