Contractile effects and receptor distributions for endothelin-1 (ET-1) in human and animal airways.
ET-1 caused concentration-dependent, sustained contraction of all airway preparations tested and was most potent in mouse trachea, with rat trachea, human bronchus and guinea-pig trachea approximately 5, 10 and 70 fold less sensitive respectively. Human non-asthmatic and asthmatic bronchi were approximately equi-sensitive to ET-1. Quantitative light microscopic autoradiography demonstrated high levels of specific [125I]-ET-1 binding sites in airway smooth muscle of rat trachea greater than human asthmatic bronchus = human non-asthmatic bronchus greater than mouse trachea much greater than guinea-pig trachea. High levels of specific ET-1 binding were also revealed in peripheral airways and in alveolar wall tissue in human, rat and mouse lung. In a limited sample of asthmatic airway smooth muscle ET-1 receptor function and density was not elevated.
Goldie
R G
RG
Department of Pharmacology, University of Western Australia, Perth, Nedlands.
Henry
P J
PJ
Paterson
J W
JW
Preuss
J M
JM
Rigby
P J
PJ
D000818:Animals; D001249:Asthma / Q000378:metabolism / Q000503:physiopathology; D001345:Autoradiography; D001665:Binding Sites; D001980:Bronchi / Q000378:metabolism / Q000502:physiology* / Q000503:physiopathology; D016232:Endothelins / Q000378:metabolism; D006168:Guinea Pigs; D006801:Humans; D066298:In Vitro Techniques; D051379:Mice; D009130:Muscle, Smooth / Q000378:metabolism; D051381:Rats; D011956:Receptors, Cell Surface / Q000378:metabolism*; D017466:Receptors, Endothelin; D012016:Reference Values; D014132:Trachea / Q000378:metabolism / Q000502:physiology* / Q000503:physiopathology
D016232:Endothelins; D011956:Receptors, Cell Surface; D017466:Receptors, Endothelin