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[α-氮杂环烷羧酸衍生物的麻醉和抗心律失常活性与其对双层磷脂膜通透性的影响之间的关系]

[Relationship of the anesthetizing and antiarrhythmic activity of alpha-azacycloalkane carboxylic acid derivatives to their effect on the permeability of a bilayer phospholipid membrane].

作者信息

Cherniakova I V

出版信息

Biull Eksp Biol Med. 1982 Aug;94(8):56-8.

PMID:7126857
Abstract

The effect of aromatic amides of N-substituted alpha-azacycloalkanecarbonic acids on electric conductivity of the bilayer phospholipid membrane was studied. The relationship between anesthetic activity of the test compounds and changes in membrane permeability was found. The most membrano-tropic compounds in the series were shown to have pronounced antiarrhythmic activity. Antiarrhythmic action of the new compounds was found to correlate with their effect on electric resistance of the bilayer phosphatidylcholine membrane. It is suggested that the regularities discovered are of importance for understanding the mechanisms of action of the compounds and for search for new agents with anesthetic and antiarrhythmic activity in the series of aromatic amides of N-substituted alpha-azacycloalkanecarbonic acids.

摘要

研究了N-取代α-氮杂环烷羧酸的芳酰胺对双层磷脂膜电导率的影响。发现了测试化合物的麻醉活性与膜通透性变化之间的关系。该系列中最具膜亲和性的化合物显示出明显的抗心律失常活性。发现新化合物的抗心律失常作用与其对双层磷脂酰胆碱膜电阻的影响相关。有人认为,所发现的规律对于理解这些化合物的作用机制以及在N-取代α-氮杂环烷羧酸的芳酰胺系列中寻找具有麻醉和抗心律失常活性的新药物具有重要意义。

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