Enhancement of local anaesthesia action by organic acid salts. (II): Aspect of kinetics in the claw nerve membrane of crayfish.
The anaesthetic action of procaine on the crayfish claw nerve was studied electrophysiologically. The onset time of conduction block (block time) was shortened and the minimum dose of procaine required for the blockade was significantly reduced in the presence of monocarboxylate anions. To investigate the mechanism of this anaesthetic enhancement, the action of procaine was considered on the basis of a simple Langmuir-type adsorption model. Rate constants in the model were estimated by observing the time course of procaine desorption from the nerve using the UV light absorption technique. The dependence of block time on procaine concentration which was simulated from the model corresponded quite well to the electrophysiological data. The model suggested the following two points. 1. The anaesthetic enhancement by some organic anions could be explained by the acceleration of procaine adsorption and lowering of the critical adsorption ratio. 2. The maximum adsorption of procaine observed was about 40 mumol per 1 g wet weight of the nerve, the value of which corresponded to 1:1 adsorption of procaine to phospholipids in the membrane.
D000200:Action Potentials / Q000187:drug effects; D000327:Adsorption; D000818:Animals; D000838:Anions / Q000494:pharmacology; D003400:Astacoidea; D002264:Carboxylic Acids / Q000494:pharmacology*; D007700:Kinetics; D008954:Models, Biological; D009431:Neural Conduction / Q000187:drug effects*; D009474:Neurons / Q000187:drug effects / Q000378:metabolism* / Q000502:physiology; D011343:Procaine / Q000493:pharmacokinetics* / Q000494:pharmacology; D012492:Salts / Q000494:pharmacology; D013056:Spectrophotometry, Ultraviolet; D013451:Sulfonic Acids / Q000494:pharmacology
D000838:Anions; D002264:Carboxylic Acids; D012492:Salts; D013451:Sulfonic Acids; D011343:Procaine