The role of electrostatic interactions in modulating the local anaesthetic effects of amphipathic agents in frog skeletal muscle.
The local anaesthetic effect of cationic, anionic, and neutral alkyl amphipathic agents was similarly enhanced in an apparently nonspecific way by circumstances which modulate electrostatic interactions (acidity, modification of charged groups at the sarcolemmal surface by group-specific reagents, or changes in the calcium concentration), presumably as the result of secondary effects on the conformation of membrane proteins. However, the selective enhancement of the local anaesthetic effect of alkyl trimethylammonium compounds by perchlorate implies a more specific interaction which may influence the penetration of hydrophobic groups into the membrane interior.
D000200:Action Potentials / Q000187:drug effects; D000476:Alkanesulfonates / Q000494:pharmacology; D017738:Alkanesulfonic Acids; D000779:Anesthetics, Local / Q000494:pharmacology*; D000818:Animals; D001001:Anura; D001566:Benzocaine / Q000494:pharmacology; D004594:Electrophysiology; D006863:Hydrogen-Ion Concentration; D066298:In Vitro Techniques; D009119:Muscle Contraction / Q000187:drug effects; D009132:Muscles / Q000187:drug effects*; D000442:Octanols / Q000494:pharmacology; D011343:Procaine / Q000494:pharmacology; D000644:Quaternary Ammonium Compounds / Q000494:pharmacology
D000476:Alkanesulfonates; D017738:Alkanesulfonic Acids; D000779:Anesthetics, Local; D000442:Octanols; D000644:Quaternary Ammonium Compounds; C042006:octyltrimethylammonium; D011343:Procaine; C042005:1-octanesulfonic acid; D001566:Benzocaine