Magnesium sulfate enhances non-depolarizing muscle relaxant vecuronium action at adult muscletype nicotinic acetylcholine receptor in vitro  

作　　者：Hong WANG Qi-sheng LIANG Lan-ren CHENG Xiao-hong LI Wei FU Wen-tao DAI Shi-tong LI 

机构地区：[1]Department of Anesthesiology, the First Affiliated Hospital of Bengbu Medical College, Bengbu 233000, China [2]Department of Anesthesiology, First People＇s Hospital, School of Medicine, Shanghai Jiaotong University, Shanghai 200030, China

出　　处：《Acta Pharmacologica Sinica》2011年第12期1454-1459,共6页中国药理学报（英文版）

基　　金：This work was supported by the National Natural Science Foundation of China （No_ 30571796）.

摘　　要：Aim： To investigate the effect of magnesium sulfate and its interaction with the non-depolarizing muscle relaxant vecuronium at adult muscle-type acetylcholine receptors in vitro. Methods： Adult muscle-type acetylcholine receptors were expressed in HEK293 cells. Drug-containing solution was applied via a gravity-driven perfusion system. The inward currents were activated by brief application of acetylcholine （ACh）, and recorded using whole-cell voltage-clamp technique. Results： Magnesium sulfate （1-100 mmol/L） inhibited the inward currents induced ACh （10 pmol/L） in a concentration-dependent manner （IC5o=29.2 mmol/L）. The inhibition of magnesium sulfate was non-competitive. In contrast, vecuronium produced a potent inhibition on the adult muscle-type acetylcholine receptor （ICso=8.7 nmol/L） by competitive antagonism. Magnesium sulfate at the concentrations of 1, 3, and 6 mmol/L markedly enhanced the inhibition of vecuronium （10 nmol/L） on adult muscle-type acetylcholine receptors. Conclusion： Clinical enhancement of vecuronium-induced muscle relaxation by magnesium sulfate can be attributed partly to synergism between magnesium sulfate and non-depolarizing muscle relaxants at adult muscle-type acetylcholine receptors.Aim： To investigate the effect of magnesium sulfate and its interaction with the non-depolarizing muscle relaxant vecuronium at adult muscle-type acetylcholine receptors in vitro. Methods： Adult muscle-type acetylcholine receptors were expressed in HEK293 cells. Drug-containing solution was applied via a gravity-driven perfusion system. The inward currents were activated by brief application of acetylcholine （ACh）, and recorded using whole-cell voltage-clamp technique. Results： Magnesium sulfate （1-100 mmol/L） inhibited the inward currents induced ACh （10 pmol/L） in a concentration-dependent manner （IC5o=29.2 mmol/L）. The inhibition of magnesium sulfate was non-competitive. In contrast, vecuronium produced a potent inhibition on the adult muscle-type acetylcholine receptor （ICso=8.7 nmol/L） by competitive antagonism. Magnesium sulfate at the concentrations of 1, 3, and 6 mmol/L markedly enhanced the inhibition of vecuronium （10 nmol/L） on adult muscle-type acetylcholine receptors. Conclusion： Clinical enhancement of vecuronium-induced muscle relaxation by magnesium sulfate can be attributed partly to synergism between magnesium sulfate and non-depolarizing muscle relaxants at adult muscle-type acetylcholine receptors.

关 键 词：magnesium sulfate non-depolarizing muscle relaxant VECURONIUM adult muscle-type acetylcholine receptor synergism 

分 类 号：TQ460.34[化学工程—制药化工] TQ463.4