[Possible mechanism of long-term anti-arrhythmia and local anesthetic effect of quaternary ammonium compounds].
In experiments with dialized neurons of L. stagnalis mollusc the recovery of Na-current (INa) after its depression by local anesthetic trimecaine and its quaternary derivative N-ethyltrimecaine (G-88) was studied. A full recovery of INa within tens of seconds after washing off trimecaine but not G-88 was observed. The half-time for vanishing of INa use-dependent depression by G-88 was 17 minutes, and there was no substantial vanishing of tonic INa block even after an hour of G-88 washing off. A hypothesis is advanced that the long recovery time of INa is one of the mechanisms providing long pharmacological action of quaternary antiarrhythmic and local anesthetic ammonium compounds.
D000083:Acetanilides / Q000494:pharmacology*; D000779:Anesthetics, Local; D000818:Animals; D000889:Anti-Arrhythmia Agents; D066298:In Vitro Techniques; D007473:Ion Channels / Q000187:drug effects; D008195:Lymnaea; D008564:Membrane Potentials / Q000187:drug effects; D009474:Neurons / Q000187:drug effects* / Q000502:physiology; D000644:Quaternary Ammonium Compounds / Q000494:pharmacology; D012964:Sodium / Q000378:metabolism; D014288:Trimecaine / Q000031:analogs & derivatives / Q000494:pharmacology*
D000083:Acetanilides; D000779:Anesthetics, Local; D000889:Anti-Arrhythmia Agents; D007473:Ion Channels; D000644:Quaternary Ammonium Compounds; C053236:N-ethyltrimecaine; D012964:Sodium; D014288:Trimecaine
O vozmozhnom mekhanizme dlitel'nogo antiaritmicheskogo i mestnoanesteziruiushchego deĭstviia chetvertichnykh ammonievykh soedineniĭ.