Jedicke U, Haller R, Koppenhöfer E
Pharmazeutischen und dem Physiologischen Institute der Christian-Albrechts-Universität, Kiel.
Arzneimittelforschung. 1988 Jun;38(6):801-5.
Effects of Aminobenzoic Acid Derivatives on the Ionic Currents in Myelinated Nerve/1st Communication: Dose-response curves Derivatives of aminobenzoic acid were modified and their blocking potencies on the ionic currents of single potential clamped myelinated nerve fibres were tested by means of dose-response curves. Starting from metacaine (ethyl m-aminobenzoate), derivatives of different basicity were produced by N-dimethylization, N-quarternization and by preparing a corresponding aliphatic amine. The corresponding free acids and the structural isomers of metacaine were tested as well. The physico-chemical properties of the derivatives were characterized by their pKa-values and their octanol/water partition coefficients. Our findings suggest that the site of action of the aminobenzoic acids tested is located at the inside of the nerve membrane. Moreover, no indications of binding to a receptor in a pharmacological sense were found.
氨基苯甲酸衍生物对有髓神经离子电流的影响/首次通讯:剂量-反应曲线 对氨基苯甲酸衍生物进行了修饰,并通过剂量-反应曲线测试了它们对单根电压钳制有髓神经纤维离子电流的阻断效力。从间卡因(间氨基苯甲酸乙酯)开始,通过N-二甲基化、N-季铵化以及制备相应的脂肪胺来制备不同碱性的衍生物。还测试了相应的游离酸和间卡因的结构异构体。这些衍生物的物理化学性质通过其pKa值和辛醇/水分配系数来表征。我们的研究结果表明,所测试的氨基苯甲酸的作用位点位于神经膜内部。此外,未发现有药理学意义上与受体结合的迹象。