Open channel and competitive block of nicotinic receptors by pancuronium and atracurium.
Open channel and competitive block of nicotinic receptors by pancuronium and atracurium.
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泮库溴铵和阿曲库铵打开通道并竞争性阻断烟碱受体。
DOI：
10.1016/s0014-2999(00)00836-0
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发表时间：
2001
影响因子：
5
通讯作者：
J. Bufler
中科院分区：
文献类型：
--
作者：
C. V. Löwenick;K. Krampfl;H. Schneck;E. Kochs;J. Bufler
用小鼠肌管研究了非去极化神经肌肉阻滞药泮库溴铵和阿曲库铵对胚胎型烟碱乙酰胆碱受体通道的作用。使用膜片钳技术结合用于在外向膜片处超快速溶液交换的装置进行实验。应用0.1 mM乙酰胆碱导致快速电流瞬变。当达到峰值振幅时，由于减敏，电流呈单指数衰减。用药后（1）阻断剂与乙酰胆碱合用后，可阻断胚胎型烟碱型乙酰胆碱受体通道，其特征是电流衰减时间常数减小;（2）在体外预孵育后，泮库溴铵或阿曲库铵竞争性阻断胚胎型烟碱乙酰胆碱受体通道。用各自的阻滞剂进行修补。观察到泮库溴铵（KB <$0.01 μM）和阿曲库铵（KB <$1 μM）对胚胎型烟碱乙酰胆碱受体通道的不同亲和力。
Mouse myotubes were used to investigate effects of the nondepolarizing neuromuscular blocking drugs pancuronium and atracurium on embryonic-type nicotinic acetylcholine receptor channels. Experiments were performed using patch-clamp techniques in combination with devices for ultra-fast solution exchange at outside–out patches. Application of 0.1 mM acetylcholine resulted in a fast current transient. When the peak amplitude was achieved, the current decayed monoexponentially due to desensitization. After application of drugs (pancuronium or atracurium), two different mechanisms of block were observed: (1) open channel block of embryonic-type nicotinic acetylcholine receptor channels after coapplication of blocker and acetylcholine, characterized by decrease of the time constant of current decay; (2) competitive block of embryonic-type nicotinic acetylcholine receptor channels by pancuronium or atracurium after preincubation of outside–out patches with the respective blocker. Different affinities of pancuronium (KB≈0.01 μM) and atracurium (KB≈1 μM) to embryonic-type nicotinic acetylcholine receptor channels were observed.
人血浆中阿曲库铵的体外降解。
影响因子：
9.8
作者：
Stiller,RL;Cook,DR;Chakravorti,S
通讯作者：
Chakravorti,S