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目的研究罗库溴铵和维库溴铵及其混合应用对骨骼肌细胞膜上成人型乙酰胆碱受体(ε-nAChR)和胎儿型乙酰胆碱受体(γ-nAChR)的作用。方法先在HEK293细胞膜上,应用脂质体转染技术表达ε-nAChR和γ-nAChR,再用全细胞膜片钳技术,比较罗库溴铵和维库溴铵及其混合应用对ε-nAChR和γ-naAChR引起峰电流的影响。结果维库溴铵和罗库溴铵均能竞争性抑制乙酰胆碱对ε-nAChR和γ-nAChR的激动作用。罗库溴铵和维库溴铵抑制ε-nAChR的半数有效抑制浓度(IC50)为169.2±12.5和(8.3±2.7)μmol/L(P<0.01),抑制γ-nAChR的IC50分别为8.6±2.7和(55.0±10.4)μmol/L(P<0.05)。两药混合应用抑制ε-nAChR的IC50为(0.7±0.3)/μmol/L;抑制γ-nAChR的IC50为(36.3±14.2)μmol/L。结论罗库溴铵对γ-nAChR的抑制作用比对ε-nAChR的作用强,而维库溴铵的作用正相反;对于ε-nAChR罗库溴铵的效能低于维库溴铵,而对γ-nAChR作用则相反;两药混合后对ε-nAChR是协同作用,对γ-nAChR却是相加作用。
Objective To investigate the effects of rocuronium and vecuronium and their combination on adult acetylcholine receptor (ε-nAChR) and fetal type acetylcholine receptor (γ-nAChR) on skeletal muscle cell membrane. Methods Eukaryotic expression vectors of ε-nAChR and γ-nAChR were transfected into HEK293 cells by whole cell patch clamp technique. The effects of rocuronium, vecuronium and their combination on ε-nAChR and γ- γ-naAChR caused by the impact of peak current. Results Both vecuronium and rocuronium competitively inhibited the agonistic effect of acetylcholine on ε-nAChR and γ-nAChR. The IC50 values of rocuronium and vecuronium for inhibition of ε-nAChR were 169.2 ± 12.5 and 8.3 ± 2.7 μmol / L, respectively (P <0.01). The IC50 of inhibition of γ-nAChR were 8.6 ± 2.7 and (55.0 ± 10.4) μmol / L (P <0.05). The IC50 of inhibition of ε-nAChR by the combination of the two drugs was (0.7 ± 0.3) / μmol / L and that of the inhibition of γ-nAChR was (36.3 ± 14.2) μmol / L. Conclusion The inhibitory effect of rocuronium on γ-nAChR is stronger than that on ε-nAChR, whereas the effect of vecuronium is reversed; the efficacy of rocuronium for ε-nAChR is less than vecuronium, The effect of γ-nAChR is opposite; the two drugs are synergistic to ε-nAChR and additive to γ-nAChR.