Stankovicová T, Stolc S, Csöllei J, Benes L
Department of Pharmacology and Toxicology, Faculty of Pharmacy, Comenius University, Bratislava, Slovak Republic.
Pharmazie. 1995 Sep;50(9):622-3.
The optically active isomers of carbisocaine [1-methyl-2-diethylaminoethyl ester of 2-(n)-heptyloxycarbonilic acid] were prepared. The blocking activity of equimolar concentrations of the carbisocaine and its corresponding enantiomers was tested on isolated rat sciatic nerves. There were no significant differences between the anesthetic action of racemic form and enantiomers, however, lower activity for the (--)-enantiomer was observed. The results may indicate negligible stereoselectivity of action of highly lipophilic local anesthetic carbisocaine in the excitable membrane.
制备了卡比佐卡因[2-(正)-庚氧基羰基酸的1-甲基-2-二乙氨基乙酯]的旋光异构体。在离体大鼠坐骨神经上测试了等摩尔浓度的卡比佐卡因及其相应对映体的阻断活性。消旋体和对映体的麻醉作用之间没有显著差异，然而，观察到(-)-对映体的活性较低。结果可能表明，高亲脂性局部麻醉药卡比佐卡因在可兴奋膜中的作用立体选择性可忽略不计。
