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

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...

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Published in中国药理学报:英文版 Vol. 32; no. 12; pp. 1454 - 1459
Main Author Hong WANG Qi-sheng LIANG Lan-ren CHENG Xiao-hong LI Wei FU Wen-tao DAI Shi-tong LI
Format Journal Article
LanguageEnglish
Published 2011
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Summary: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.
Bibliography: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.
magnesium sulfate; non-depolarizing muscle relaxant; vecuronium; adult muscle-type acetylcholine receptor; synergism
31-1347/R
ISSN:1671-4083
1745-7254