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γ-氨基丁酸和哌嗪对龙虾肌纤维及青蛙脊髓作用的比较研究。

A comparative study of the action of gamma-aminobutyric acid and piperazine on the lobster muscle fibre and the frog spinal cord.

作者信息

Constanti A, Nistri A

出版信息

Br J Pharmacol. 1976 Jul;57(3):347-58. doi: 10.1111/j.1476-5381.1976.tb07673.x.

Abstract

1 The effects of gamma-aminobutyric acid (GABA) and piperazine were compared on two in vitro preparations, the lobster muscle fibre and the frog spinal cord. 2 Both GABA and piperazine increased the membrane conductance of single lobster muscle fibres without changing the membrane potential; sigmoidal log dose-conductance curves for these agents were obtained and a similar model expressed the receptor interaction of both substances. 3 The actions of GABA and piperazine on lobster muscle were antagonized by picrotoxin and were Cl-dependent. 4 In the frog spinal cord GABA depolarized the dorsal roots presumably by mimicking the activity of the transmitter depolarizing the primary afferents; sigmoidal log dose-response curves for GABA were obtained. 5 On the dorsal roots piperazine produced either depolarizations or biphasic responses; these were mainly indirect effects as was shown by experiments in the presence of tetrodotoxin (TTX). 6 The effects of GABA on the dorsal root (in TTX-treated cords) were antagonized by picrotoxin whereas those of piperazine were more resistant to this alkaloid. The GABA-induced responses appeared to be largely Na+-dependent while both Na+ and Cl- seemed to mediate the effects of piperazine. 7 It is proposed that piperazine has GABA-agonist activity on lobster muscle but little GABA-like activity on the frog spinal cord.

摘要
  1. 比较了γ-氨基丁酸(GABA)和哌嗪对两种体外制备物的作用,即龙虾肌肉纤维和青蛙脊髓。2. GABA和哌嗪均增加了单个龙虾肌肉纤维的膜电导,而不改变膜电位;获得了这些药物的S形对数剂量-电导曲线,并且一个相似的模型表达了这两种物质的受体相互作用。3. GABA和哌嗪对龙虾肌肉的作用被印防己毒素拮抗,且依赖于氯离子。4. 在青蛙脊髓中,GABA可能通过模拟使初级传入纤维去极化的递质的活性,使背根去极化;获得了GABA的S形对数剂量-反应曲线。5. 在背根上,哌嗪产生去极化或双相反应;如在存在河豚毒素(TTX)的实验所示,这些主要是间接效应。6. GABA对背根(在经TTX处理的脊髓中)的作用被印防己毒素拮抗,而哌嗪的作用对这种生物碱更具抗性。GABA诱导的反应似乎很大程度上依赖于钠离子,而钠离子和氯离子似乎都介导了哌嗪的作用。7. 有人提出,哌嗪对龙虾肌肉具有GABA激动剂活性,但对青蛙脊髓几乎没有GABA样活性。

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The effects of piperazine on rat sympathetic neurones.哌嗪对大鼠交感神经元的作用。
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本文引用的文献

1
MECHANISM OF THE PARALYSING ACTION OF PIPERAZINE ON ASCARIS MUSCLE.哌嗪对蛔虫肌肉的麻痹作用机制
Br J Pharmacol Chemother. 1964 Jun;22(3):463-77. doi: 10.1111/j.1476-5381.1964.tb01701.x.
2
A MOLECULAR BASIS FOR DRUG ACTION.药物作用的分子基础。
J Pharm Pharmacol. 1964 Mar;16:137-57. doi: 10.1111/j.2042-7158.1964.tb07437.x.
4
A modification of receptor theory.受体理论的一种修正。
Br J Pharmacol Chemother. 1956 Dec;11(4):379-93. doi: 10.1111/j.1476-5381.1956.tb00006.x.
5
The electrical constants of Purkinje fibres.浦肯野纤维的电学常数。
J Physiol. 1952 Nov;118(3):348-60. doi: 10.1113/jphysiol.1952.sp004799.
10
Piperazine neurotoxicity: "worm wobble".哌嗪神经毒性:“蠕虫摆动”
Br Med J. 1971 Dec 25;4(5790):792. doi: 10.1136/bmj.4.5790.792.

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