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[1-金刚烷基自由基对箭毒样活性的影响]

[The effect of 1-adamantyl radicals on curare-like activity].

作者信息

Kharkevich D A, Skoldinov A P

出版信息

Biull Eksp Biol Med. 1975 May;79(5):71-5.

PMID:132205
Abstract

In the series of polymethylene bis-ammonium salts R(CH3)2N(CH2)NN(CH3)2R . 2I--(R=CH3 or Ad) a study was made of the significance of hydrophobic 1-adamantyle radicals (1--Ad) for curare-like activity. Administration of 1-ad radicals into the cation groups of depolarizing agents (n-9--11) altered their mechanism of action and diminished their activity. Attachmeni of 1-Ad radicals to the both quarternary nitrogen atoms of the antidepolarizing agents (n=5 and 6) sharply increased their curare-like activity. The data obtained pointed to the presence of hydrophobic zones in the cholinoreceptors of skeletal muscles.

摘要

在聚亚甲基双铵盐系列R(CH₃)₂N(CH₂)NN(CH₃)₂R·2I⁻(R = CH₃或Ad)中,研究了疏水性1-金刚烷基团(1-Ad)对箭毒样活性的意义。将1-Ad基团引入去极化剂的阳离子基团(n = 9 - 11)中会改变其作用机制并降低其活性。将1-Ad基团连接到抗去极化剂的两个季氮原子上(n = 5和6)会显著提高其箭毒样活性。所获得的数据表明骨骼肌胆碱能受体中存在疏水区。

相似文献

1
[The effect of 1-adamantyl radicals on curare-like activity].[1-金刚烷基自由基对箭毒样活性的影响]
Biull Eksp Biol Med. 1975 May;79(5):71-5.
2
[Curare-like activity of quaternary ammonium compounds containing 2-adamantyl radicals].[含2-金刚烷基的季铵化合物的箭毒样活性]
Farmakol Toksikol. 1981 Nov-Dec;44(6):670-2.
3
[Role of the hydrophobicity of polymethylene-bis-quaternary ammonium compounds in the mechanism of their curare-like action].[聚亚甲基双季铵化合物的疏水性在其箭毒样作用机制中的作用]
Farmakol Toksikol. 1976 Jan-Feb;39(1):21-5.
4
[A nondepolarizing muscle relaxant with rapidly developing and short-term action].一种具有快速起效和短效作用的非去极化肌松药。
Eksp Klin Farmakol. 1998 Sep-Oct;61(5):18-20.
5
[Use of a magnetic field for guided transport of curare-like substances].[利用磁场引导箭毒样物质的运输]
Farmakol Toksikol. 1985 Sep-Oct;48(5):32-5.
6
[Curare-like activity of decadonium diiodide].[二碘化十烃季铵的箭毒样活性]
Farmakol Toksikol. 1970 Jul-Aug;33(4):395-9.
7
[The effect of adamantyl radicals on the mechanism of the cholinergic action of mono-quaternary ammonium compounds].[金刚烷基对单季铵化合物胆碱能作用机制的影响]
Farmakol Toksikol. 1973 Mar-Apr;36(2):201-5.
8
[The effect of adamantyl radicals on the mechanism of the cholinergic action of mono-quaternary ammonium compounds].
Farmakol Toksikol. 1973 Mar-Apr;36(2):201-5.
9
[Effect of adamantyl quaternary ammonium derivatives on the autonomic ganglia].
Farmakol Toksikol. 1987 Nov-Dec;50(6):37-41.
10
[Pharmacodynamic evaluation of a new synthetic curare-like agent: acetylenic-gallamine].一种新型合成箭毒样药物:乙炔基加拉明的药效学评价
Arch Int Pharmacodyn Ther. 1970 Mar;184(1):75-92.