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Eur J Pharmacol ; 569(1-2): 37-40, 2007 Aug 13.
Article in English | MEDLINE | ID: mdl-17588565

ABSTRACT

Neuromuscular blocking drugs produce muscle weakness by interaction with nicotinic-acetylcholine receptors. Cardiovascular side effects have been reported. In this study the neuromuscular blocking drug vecuronium and the controls gallamine and pancuronium slowed the rate of atropine induced [(3)H]N-methylscopolamine dissociation from Chinese hamster ovary cells expressing recombinant human muscarinic M2 receptors K(off) values min(-1); vecuronium (125 nM), atropine 0.45+/-0.07+blocker 0.04+/-0.02; gallamine (21 nM), atropine 0.42+/-0.05+blocker 0.15+/-0.04; pancuronium(21 nM), atropine 0.36+/-0.03+blocker 0.03+/-0.01). These data indicate that vecuronium, gallamine and pancuronium interact with an allosteric site on the muscarinic M2 receptor (located on the heart) and this may explain some of their cardiac side effects.


Subject(s)
Neuromuscular Blocking Agents/pharmacology , Pancuronium/pharmacology , Receptor, Muscarinic M2/metabolism , Vecuronium Bromide/pharmacology , Allosteric Regulation/drug effects , Animals , Atropine/pharmacology , Binding, Competitive/drug effects , CHO Cells , Cricetinae , Cricetulus , Gallamine Triethiodide/pharmacology , Humans , Kinetics , Muscarinic Antagonists/pharmacology , N-Methylscopolamine/metabolism , Pancuronium/metabolism , Radioligand Assay , Receptor, Muscarinic M2/antagonists & inhibitors , Receptor, Muscarinic M2/genetics , Recombinant Proteins/metabolism , Tritium
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