Cardi P, Lartigue M, Meunier J M
Laboratoire de Physiologie, UER de Médecine et de Pharmacie, Limoges, France.
J Pharm Pharmacol. 1988 Mar;40(3):181-4. doi: 10.1111/j.2042-7158.1988.tb05214.x.
The depolarizing effect of various local anaesthetics (LA) on the membrane potential of Helix central neurons has been examined. There is a relation between depolarizing effect and concentration of LA in the bath that is linear over a range of concentrations. The slope of the curve is significantly higher for amethocaine (tetracaine) than for procaine while for dibucaine the dose-response relation is not linear. The blockade of a response to acetylcholine (ACh) is about two fold higher for dibucaine and amethocaine than for procaine. These results suggest that both amethocaine and procaine act at the ACh-site in addition to their binding with specific sites located within the ionic channel lumen; dibucaine appears to act through another mechanism.