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

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Abstract
Although ET1 and ET2 binding sites were found in rat lung membranes, a selective ET1 receptor antagonist, BQ-123 (10 μm), 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 μm) 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.