Skeletal muscle relaxants inhibit rat tracheal smooth muscle tone in vitro.
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Milchert M, Spassov A, Meissner K, Nedeljkov V, Lehmann C, Wendt M, Loster BW, Mazurkiewicz-Janik M, Gedrange T, Pavlovic D
Skeletal muscle relaxants inhibit rat tracheal smooth muscle tone in vitro.
J Physiol Pharmacol. 2009 Dec;60 Suppl 8:5-11.
- PubMed ID
- 20400785 [ View in PubMed]
- Abstract
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. The NMBDs produced relaxation in the preparations precontracted with CARB or PILO. The order of potency after CARB (10(-6)M) was (EC(50)): 4-DAMP (9.8) >atropine (9.2) >methoctramine (6.4) >pancuronium (6.0) >mivacurium (5.8) >cisatracurium (5.6) >gallamine (5.2) >rocuronium (4.8) >succinylcholine (2.9); NMBDs also partially prevented contraction elicited by the electrical field stimulation. We demonstrated that the clinically used NMBD that were examined produced rat TSM relaxation, probably by predominantly blocking postjunctional muscarinic receptors.
DrugBank Data that Cites this Article
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Pancuronium Muscarinic acetylcholine receptor M2 Protein Humans UnknownAntagonistDetails Pancuronium Muscarinic acetylcholine receptor M3 Protein Humans UnknownAntagonistDetails Rocuronium Muscarinic acetylcholine receptor M2 Protein Humans YesAntagonistDetails