The effect of different non-depolarizing muscle relaxants (gallamine, pancuronium, vecuronium, D-tubocurarine) on [3H]norepinephrine release in response to electrical stimulation was studied in isolated guinea-pig atrium. High pressure liquid chromatography combined with electrochemical and radiochemical detection revealed that the released radioactivity was mainly in the form of [3H]norepinephrine release. Oxotremorine, a pure muscarinic agonist, reduced the release of tritium. Gallamine and pancuronium, like atropine, prevented the inhibitory effect of oxotremorine. D-Tubocurarine and vecuronium had no such effect. These findings indicate that gallamine and pancuronium exert a presynaptic antimuscarinic, atropine-like effect, by inhibiting muscarinic receptors located on the axon terminals of sympathetic neurons thereby enhancing norepinephrine release. It is suggested that this phenomenon might play some role in tachycardia observed during surgical anaesthesia when gallamine or pancuronium have been administered.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/0165-1838(87)90134-2 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Efficient Reversal of Neuromuscular Blocking Agent-Induced Biological Functions and Side Effects by an Extended Biphen[3]arene Carboxylate.
J Med Chem
December 2024
State Key Laboratory of National Security Specially Needed Medicines, Beijing Institute of Pharmacology and Toxicology, Beijing 100850, P. R. China.
Article Synopsis
- * A new compound called ExBP3C was developed as an effective reversal agent for multiple NMBAs, showing strong binding capabilities with agents like atracurium and rocuronium.
- * ExBP3C demonstrated better efficiency than the existing reversal drug sugammadex, and in tests, it rapidly corrected heart rate issues caused by an overdose of atracurium within two minutes, indicating good safety and biocompatibility.
Neuroactive steroids, WIN-compounds and cholesterol share a common binding site on muscarinic acetylcholine receptors.
Biochem Pharmacol
October 2021
Institute of Physiology, Czech Academy of Sciences, Prague, Czech Republic. Electronic address:
Endogenous neurosteroids and their synthetic analogues-neuroactive steroids-have been found to bind to muscarinic acetylcholine receptors and allosterically modulate acetylcholine binding and function. Using radioligand binding experiments we investigated their binding mode. We show that neuroactive steroids bind to two binding sites on muscarinic receptors.
View Article and Find Full Text PDFErroneous neuraxial administration of neuromuscular blocking drugs: Clinical and human factors analysis.
Eur J Anaesthesiol
October 2020
From the Department of Anaesthesia, Tawam Hospital, Al Ain, Abu Dhabi, UAE.
Background: Drug errors during neuraxial anaesthesia or analgesia are not well known.
Objectives: To review the clinical consequences associated with incorrect administration of neuromuscular blocking drugs (NMBDs) during spinal or epidural anaesthesia, and to investigate human factors and strategies available to help prevent such errors.
Design: A review of reports of neuraxial administration of NMBDs in humans.
Skeletal muscle relaxants inhibit rat tracheal smooth muscle tone in vitro.
J Physiol Pharmacol
December 2009
Department of Anesthesiology and Intensive Care Medicine, Ernst Moritz Arndt University, Greifswald, Germany.
Neuromuscular blocking drugs (NMBD) can inhibit not only nicotinic but also muscarinic (M) receptors and thereby affect not only skeletal but also smooth muscle (SM) tone. A selective postjunctional muscarinic inhibition would relax, while prejunctional inhibition of muscarinic M2 receptor might hasten SM contraction thereby increasing the risk of bronchospasm. In rat tracheal rings in vitro we evaluated the effects of cumulative concentrations of some NMBD and M receptor blocking agents for their effects on tracheal smooth muscle (TSM) tone pre-contracted with carbachol (CARB; 5 x 10(-7)M or 10(-6)M), pilocarpine (PILO; 5 x 10(-6)M), or by electrical field stimulation.
View Article and Find Full Text PDFAllosteric interaction of the neuromuscular blockers vecuronium and pancuronium with recombinant human muscarinic M2 receptors.
Eur J Pharmacol
August 2007
Department of Cardiovascular Sciences (Pharmacology and Therapeutics Group), Division of Anaesthesia, Critical Care and Pain Management, University of Leicester, Leicester Royal Infirmary, Leicester, LE1 5WW, UK.
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.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!