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Human big‐endothelin‐1 and endothelin‐1 release prostacyclin via the activation of ET 1 receptors in the rat perfused lung
Author(s) -
D'OrléansJuste Pedro,
Télémaque Sabine,
Claing Audrey,
Ihara Masaki,
Yano Mitsuo
Publication year - 1992
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1992.tb09055.x
Subject(s) - prostacyclin , endothelin receptor , receptor , endothelin 1 , endocrinology , medicine , endothelins , chemistry , antagonist , endothelin 3 , lung , receptor antagonist , biology
Although ET 1 and ET 2 binding sites were found in rat lung membranes, a selective ET 1 receptor antagonist, BQ‐123 (10 μ m ), did not displace [ 125 I]‐endothelin‐1 ([ 125 I]ET‐1) from ET 2 sites, illustrating the selectivity of the angatonist for ET 1 receptors. In rat perfused lungs, BQ‐123 (1 μ m ) markedly reduced the prostacyclin (PGI 2 ) releasing properties of endothelin‐1 (ET‐1: 5 n m ) and human big‐ET‐1 (100 n m ) suggesting that both peptides induce the release of PGI 2 via the selective activation of ET 1 receptors.