Yoneda I, Sakuta H, Okamoto K, Watanabe Y
Department of Pharmacology, National Defense Medical College, Saitama, Japan.
Eur J Pharmacol. 1993 Nov 15;247(3):267-72. doi: 10.1016/0922-4106(93)90194-e.
Effects of local anesthetics and structurally related drugs on the glibenclamide-sensitive K+ currents evoked by Y-26763 (a K+ channel opener) were investigated in native Xenopus oocytes. The K+ current induced by Y-26763 (100 microM) was reversibly suppressed by all six local anesthetics tested in a concentration-dependent manner with the rank order of potencies (IC50 in microM): bupivacaine (67) > dibucaine (136) > tetracaine (845) > lidocaine (1710) = mepivacaine (1945) > procaine (3112). (+)-Propranolol and mexiletine also suppressed Y-26763-induced K+ currents with IC50 values of 115 microM and 789 microM, respectively. These results suggest that a suppressive action on glibenclamide-sensitive K+ channels is the common property of local anesthetics.
在非洲爪蟾卵母细胞中研究了局部麻醉药及结构相关药物对Y - 26763（一种钾通道开放剂）诱发的格列本脲敏感钾电流的影响。Y - 26763（100微摩尔）诱导的钾电流被所测试的全部六种局部麻醉药以浓度依赖性方式可逆性抑制，其效价顺序（IC50，单位为微摩尔）为：布比卡因（67）> 丁卡因（136）> 丁哌卡因（845）> 利多卡因（1710）= 甲哌卡因（1945）> 普鲁卡因（3112）。（+）-普萘洛尔和美西律也抑制Y - 26763诱导的钾电流，IC50值分别为115微摩尔和789微摩尔。这些结果表明，对格列本脲敏感钾通道的抑制作用是局部麻醉药的共同特性。
