P. Dorleansjuste et al., HUMAN BIG-ENDOTHELIN-1 AND ENDOTHELIN-1 RELEASE PROSTACYCLIN VIA THE ACTIVATION OF ET1 RECEPTORS IN THE RAT PERFUSED LUNG, British Journal of Pharmacology, 105(4), 1992, pp. 773-775
Although ET1 and ET2 binding sites were found in rat lung membranes, a
selective ET1 receptor antagonist, BQ-123 (10-mu-M), did not displace
[I-125]-endothelin-1 ([I-125]ET-1) from ET2 sites, illustrating the s
electivity of the angatonist for ET1 receptors. In rat perfused lungs,
BQ-123 (1-mu-M) markedly reduced the prostacyclin (PGI2) releasing pr
operties of endothelin-1 (ET-1:5 nM) and human big-ET-1 (100 nM) sugge
sting that both peptides induce the release of PGI2 via the selective
activation of ET1 receptors.