Human big-endothelin-1 and endothelin-1 release prostacyclin via the activation of ET1 receptors in the rat perfused lung

P D'Orléans-Juste; S Télémaque; A Claing; M Ihara; M Yano

doi:10.1111/j.1476-5381.1992.tb09055.x

Human big-endothelin-1 and endothelin-1 release prostacyclin via the activation of ET1 receptors in the rat perfused lung

Br J Pharmacol. 1992 Apr;105(4):773-5. doi: 10.1111/j.1476-5381.1992.tb09055.x.

Authors

P D'Orléans-Juste¹, S Télémaque, A Claing, M Ihara, M Yano

Affiliation

¹ Department of Pharmacology, Medical School, Université de Sherbrooke, Québec, Canada.

Abstract

Although ET1 and ET2 binding sites were found in rat lung membranes, a selective ET1 receptor antagonist, BQ-123 (10 microM), did not displace [125I]-endothelin-1 ([125I]ET-1) from ET2 sites, illustrating the selectivity of the angatonist for ET1 receptors. In rat perfused lungs, BQ-123 (1 microM) markedly reduced the prostacyclin (PGI2) releasing properties of endothelin-1 (ET-1: 5 nM) and human big-ET-1 (100 nM) suggesting that both peptides induce the release of PGI2 via the selective activation of ET1 receptors.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Endothelin-1
Endothelins / pharmacology*
Epoprostenol / metabolism*
Humans
In Vitro Techniques
Lung / drug effects*
Lung / metabolism
Male
Peptides, Cyclic / pharmacology
Protein Precursors / pharmacology*
Rats
Rats, Inbred Strains
Receptors, Cell Surface / antagonists & inhibitors
Receptors, Cell Surface / drug effects
Receptors, Cell Surface / physiology
Receptors, Endothelin

Substances

Endothelin-1
Endothelins
Peptides, Cyclic
Protein Precursors
Receptors, Cell Surface
Receptors, Endothelin
Epoprostenol
cyclo(Trp-Asp-Pro-Val-Leu)