Abstract | BACKGROUND: Neuromuscular relaxants such as pancuronium bind to M2 and M3 muscarinic receptors as antagonists. Blockade of muscarinic receptors in atria of the M2 subtype mediates tachycardia. In the lung, blockade of M2 receptors on parasympathetic nerves potentiates vagally induced bronchospasm, whereas blockade of M3 receptors on bronchial smooth muscle inhibits bronchospasm. The current study was designed to quantify the affinity of a series of neuromuscular relaxants for the M2 and M3 muscarinic receptors, which were individually stably transfected in Chinese hamster ovary cell lines. METHODS: RESULTS: All muscle relaxants evaluated displaced 3H-QNB from muscarinic receptors. The relative order of potency for the M2 muscarinic receptor (highest to lowest) was pancuronium, gallamine, rocuronium, atracurium, pipecuronium, doxacurium, mivacurium, and succinylcholine. The relative order of potency for the M3 muscarinic receptor (highest to lowest) was pancuronium, atracurium, pipecuronium, rocuronium, mivacurium, gallamine, succinylcholine, and doxacurium. CONCLUSIONS:
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Authors | V Y Hou, C A Hirshman, C W Emala |
Journal | Anesthesiology
(Anesthesiology)
Vol. 88
Issue 3
Pg. 744-50
(Mar 1998)
ISSN: 0003-3022 [Print] United States |
PMID | 9523819
(Publication Type: Journal Article)
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Chemical References |
- Neuromuscular Nondepolarizing Agents
- Receptor, Muscarinic M2
- Receptor, Muscarinic M3
- Receptors, Muscarinic
- Recombinant Proteins
- Quinuclidinyl Benzilate
- Carbachol
- Pancuronium
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Topics |
- Animals
- CHO Cells
- Carbachol
(pharmacology)
- Cell Membrane
- Cricetinae
- Neuromuscular Nondepolarizing Agents
(pharmacology)
- Pancuronium
(pharmacology)
- Quinuclidinyl Benzilate
(metabolism)
- Radioligand Assay
- Receptor, Muscarinic M2
- Receptor, Muscarinic M3
- Receptors, Muscarinic
(drug effects)
- Recombinant Proteins
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