七氟醚和异氟醚对不同浓度罗库溴铵抑制乙酰胆碱受体内向电流的影响

Effects of sevoflurane and isoflurane on different concentration of rocuronium in inhibiting inward current of acetylcholine receptors

目的探讨挥发性麻醉药七氟醚(sevoflurane)、异氟醚(isoflurane)对不同浓度罗库溴铵(rocuronium)抑制骨骼肌成人型乙酰胆碱受体(ε-nAChR)内向电流的影响。方法通过脂质体转染建立表达ε-nAChR的HEK293细胞,用全细胞膜片钳检测乙酰胆碱(ACh)激动受体峰电流。拟合七氟醚、异氟醚、罗库溴铵抑制受体的浓度效应关系(IC50)。用0.5IC50浓度的七氟醚、异氟醚预处理ε-nAChR,记录浓度为IC5、0.5 IC50、IC50的罗库溴铵对ACh诱发峰电流的抑制率。各组以单独使用相应浓度罗库溴铵作为对照。结果七氟醚、异氟醚、罗库溴铵的IC50值分别为:(824.27±14.73)μmol.L-1、(1031.53±62.91)μmol.L-1、(150.45±12.5)μmol.L-1(P<0.01)。0.5 IC50浓度的异氟醚增强IC5浓度罗库溴铵拮抗受体的作用强于七氟醚(P<0.01)。结论七氟醚、异氟醚增强罗库溴铵对ε-nAChR的阻滞作用;两种吸入麻醉药对低浓度的罗库溴铵具有更明显的协同效应,且异氟醚作用强于七氟醚。

Aim To investigate the effects of sevoflurane and isoflurane on rocuronium in inhibiting inward current of adult skeletal muscle acetylcholine receptor（ε-nAChR）.Methods ε-nAChR was expressed heterologously in HEK293 cell using liposome transfection technology.The whole cell patch clamp technology was used to establish the concentration-effect curves for the inhibition of acetylcholine（ACh）induced current and the calculation of the 50% inhibitory concentration values（IC50）respectively.The inhibitory effect of rocuronium at concentrations of IC5,0.5 IC50,IC50 was studied in the presence of the sevoflurane,isoflurane at a concentration of 0.5 IC50.The peak current was recorded by the whole cell patch clamp.Results The IC50 values was（824.27±14.73）μmol·L-1,（1031.53±62.91）μmol·L-1 and（150.45±12.5）μmol·L-1 for sevoflurane,isoflurane and rocuronium respectively.Sevoflurane and isoflurane increased the inhibition of ACh induced current amplitude in a concentration-dependent manner（P0.01）.At the concentration of 0.5 IC50 sevoflurane and isoflurane enhanced inhibition of Ach induced current amplitude by rocuronium at the concentration of IC5（P0.01）.Conclusion Coapplication of either isoflurane or sevoflurane with rocuronium significantly enhanced the inhibitory effects of rocuronium.At small concentrations,this effect of isoflurane was stronger than that of sevoflurane.