Allosteric interaction of the neuromuscular blockers vecuronium and pancuronium with recombinant human muscarinic M2 receptors.
Article Details
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Cembala TM, Forde SC, Appadu BL, Lambert DG
Allosteric interaction of the neuromuscular blockers vecuronium and pancuronium with recombinant human muscarinic M2 receptors.
Eur J Pharmacol. 2007 Aug 13;569(1-2):37-40. Epub 2007 May 22.
- PubMed ID
- 17588565 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Atropine Muscarinic acetylcholine receptor M2 Protein Humans YesAntagonistDetails Gallamine triethiodide Muscarinic acetylcholine receptor M2 Protein Humans YesAntagonistDetails Pancuronium Muscarinic acetylcholine receptor M2 Protein Humans UnknownAntagonistDetails