各种局部麻醉药对蛞蝓神经元的去极化作用：剂量-反应关系
Depolarizing effect of various local anaesthetics on the Helix aspersa neurons: dose-response relationship.
作者信息
Cardi P, Lartigue M, Meunier J M
机构信息
Laboratoire de Physiologie, UER de Médecine et de Pharmacie, Limoges, France.
出版信息
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.
已对多种局部麻醉药（LA）对耳螺中枢神经元膜电位的去极化作用进行了研究。在一定浓度范围内，去极化作用与浴槽中LA的浓度呈线性关系。丁卡因（地卡因）曲线的斜率明显高于普鲁卡因，而布比卡因的剂量-反应关系则不是线性的。布比卡因和丁卡因对乙酰胆碱（ACh）反应的阻断作用比普鲁卡因高约两倍。这些结果表明，丁卡因和普鲁卡因除了与位于离子通道腔内的特定位点结合外，还作用于ACh位点；布比卡因似乎通过另一种机制起作用。
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