title: Muscarinic M3 receptors mediate contraction of human central and peripheral airway smooth muscle.
abstract: The muscarinic receptor subtype involved in human airway smooth muscle contraction was characterised for the first time, using subtype-selective muscarinic antagonists. It was demonstrated that methacholine-induced contraction of central (trachea) and peripheral (small bronchi) airway smooth muscle preparations was antagonised by pirenzepine, AF-DX 116, 4-DAMP methobromide, hexahydrosiladifenidol, and methoctramine with pA2-values characteristic of M3 (smooth muscle/glandular) muscarinic receptors. Since these pA2-values demonstrate significant correlations with those found in bovine and guinea-pig tracheal smooth muscle contraction, it is concluded that these animal tissues provide a good model for the study of M3 subtype-selective muscarinic antagonists to be used as bronchodilators.
authors: Department of Pharmacology and Therapeutics, University of Groningen, The Netherlands.
authors: A F
authors: AF
authors: Roffel
authors: C R
authors: CR
authors: Elzinga
authors: J
authors: J
authors: Zaagsma
mesh_terms: D001980:Bronchi / Q000502:physiology*; D006801:Humans; D066298:In Vitro Techniques; D009241:Ipratropium / Q000494:pharmacology; D009119:Muscle Contraction / Q000502:physiology; D009130:Muscle, Smooth / Q000502:physiology*; D010276:Parasympatholytics / Q000494:pharmacology; D010880:Piperidines / Q000494:pharmacology; D010890:Pirenzepine / Q000031:analogs & derivatives / Q000494:pharmacology; D011976:Receptors, Muscarinic / Q000502:physiology*; D014132:Trachea / Q000502:physiology*
chemical_list: D010276:Parasympatholytics; D010880:Piperidines; D011976:Receptors, Muscarinic; D010890:Pirenzepine; C042375:4-diphenylacetoxy-1,1-dimethylpiperidinium; D009241:Ipratropium; C046773:hexahydrosiladifenidol; C048593:otenzepad