[Relationship of the anesthetizing and antiarrhythmic activity of alpha-azacycloalkane carboxylic acid derivatives to their effect on the permeability of a bilayer phospholipid membrane].
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.
D000577:Amides / Q000494:pharmacology*; D000777:Anesthetics / Q000494:pharmacology*; D000889:Anti-Arrhythmia Agents / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D006571:Heterocyclic Compounds / Q000494:pharmacology*; D008051:Lipid Bilayers / Q000494:pharmacology*; D010539:Permeability; D010743:Phospholipids / Q000494:pharmacology*; D013501:Surface-Active Agents / Q000494:pharmacology
D000577:Amides; D000777:Anesthetics; D000889:Anti-Arrhythmia Agents; D006571:Heterocyclic Compounds; D008051:Lipid Bilayers; D010743:Phospholipids; D013501:Surface-Active Agents
Sviaz' anesteziruiushcheĭ i antiaritmicheskoĭ aktivnosti proizvodnykh al'fa-azatsikloalkankarbonovykh kislot s ikh vliianiem na pronitsaemost' bisloĭnoĭ fosfolipidnoĭ membrany.