Kitamura K, Itoh T, Ueno H, Kanmura Y, Inoue R, Kuriyama H
Drugs Exp Clin Res. 1986;12(9-10):773-84.
Procaine acts on the cell membrane as a depolarizing agent. It inhibits K-conductance; as a consequence, the membrane is depolarized and the spike potential is readily generated by outward current pulses. This inhibition of the K-conductance of membrane induced by procaine is discussed in relation to the K channel classified by the patch clamp procedure. The authors' observations indicate that procaine acts as a stimulant rather than as a stabilizer of the membrane. Furthermore, procaine inhibits the release of Ca from the store site, with no effect on the contractile protein. This local anaesthetic agent acts not only on the surface membrane but also on the internal membrane, the sarcoplasmic reticulum. Procaine reduces mechanical activity and stabilization of vascular smooth muscles occurs.
普鲁卡因作为一种去极化剂作用于细胞膜。它抑制钾离子电导;因此,膜发生去极化,向外的电流脉冲很容易产生动作电位。结合膜片钳技术分类的钾通道,讨论了普鲁卡因对膜钾离子电导的这种抑制作用。作者的观察表明,普鲁卡因作为膜的刺激剂而非稳定剂起作用。此外,普鲁卡因抑制钙从储存部位的释放,对收缩蛋白无影响。这种局部麻醉剂不仅作用于表面膜,还作用于内膜,即肌浆网。普鲁卡因降低机械活性,血管平滑肌出现稳定状态。