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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。

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