Stankovicová T, Nemcek V, Stolc S
Katedra farmakológie a toxikológie Farmaceutickej fakulty Univerzity Komenského, Bratislava.
Ceska Slov Farm. 1995 Oct;44(5):265-7.
Effects of the local anaesthetic trimecaine and its quaternary derivative on the isolated rat sciatic nerves were examined. Trimecaine inhibited action potential propagation in the isolated nerve in vitro at four-times lower concentrations than its quaternary derivative. Despite extracellular application, the quaternary derivative inhibited action potential propagation in the sciatic nerve but with a longer half-life in comparison with trimecaine. With increasing external pH, the blocking effect of trimecaine was profound. The blocking potency of the quaternary compound was not consistently changed with the changes in external medium pH.
研究了局部麻醉药三甲卡因及其季铵衍生物对离体大鼠坐骨神经的作用。在体外,三甲卡因抑制离体神经动作电位传导的浓度比其季铵衍生物低四倍。尽管是细胞外应用,但该季铵衍生物仍能抑制坐骨神经动作电位的传导,不过与三甲卡因相比,其半衰期更长。随着细胞外pH值的升高,三甲卡因的阻断作用更为显著。该季铵化合物的阻断效能并不随细胞外介质pH值的变化而持续改变。