Receptors for endothelin-1 in asthmatic human peripheral lung.
[125I]-endothelin-1 ([125I]-ET-1) binding was assessed by autoradiography in peripheral airway smooth muscle and alveolar wall tissue in human non-asthmatic and asthmatic peripheral lung. Levels of specific binding to these structures were similar in both non-asthmatic and asthmatic lung. The use of the receptor subtype-selective ligands, BQ-123 (ETA) and sarafotoxin S6c (ETB), demonstrated the existence of both ETA and ETB sites in airway smooth muscle and in alveoli. In airway smooth muscle from both sources, the great majority of sites were of the ETB subtype. Quantitative analyses of asthmatic and non-asthmatic alveolar wall tissue demonstrated that 29-32% of specific [125I]-ET-1 binding was to ETA sites and 68-71% was to ETB sites. Thus, asthma was not associated with any significant alteration in the densities of ETA and ETB receptors in peripheral human lung.
Knott
P G
PG
Department of Pharmacology, University of Western Australia, Nedlands.
D'Aprile
A C
AC
Henry
P J
PJ
Hay
D W
DW
Goldie
R G
RG
D000293:Adolescent; D000328:Adult; D001249:Asthma / Q000378:metabolism*; D001345:Autoradiography; D065128:Endothelin Receptor Antagonists; D005260:Female; D006801:Humans; D008168:Lung / Q000737:chemistry* / Q000378:metabolism; D008297:Male; D010456:Peptides, Cyclic / Q000494:pharmacology; D017466:Receptors, Endothelin / Q000032:analysis* / Q000378:metabolism
D065128:Endothelin Receptor Antagonists; D010456:Peptides, Cyclic; D017466:Receptors, Endothelin; C072247:cyclo(Trp-Asp-Pro-Val-Leu)