PMID: 8587477Jan 1, 1995Paper

Characterization of endothelin receptors and endothelin-converting enzyme activity in the rabbit lung

Journal of Cardiovascular Pharmacology
J P GrattonP D'Orléans-Juste

Abstract

We had earlier shown that endothelin-1 (ET-1)-induced vasoconstriction and prostacyclin (PGI2) release in the rabbit kidney are exclusively linked to ETA receptor activation. In contrast, another study showed that ET-1 inhibited platelet aggregation ex vivo through the release of PGI2 solely via the activation of ETB receptors. In an attempt to identify the organs involved in the ET-1-induced release of PGI2 in vivo, we characterized the receptors responsible for the release of this eicosanoid and also monitored the activity of the endothelin-converting enzyme (ECE) in rabbit pulmonary lobe. In this perfused organ, a 5-min infusion of ET-1 (50 nM) triggered a marked release of PGI2 and an increase in perfusion pressure, both of which were mimicked by the selective ETB agonist IRL 1620 (0.5 microM). Furthermore, a selective ETB antagonist, BQ-788 (10 nM), markedly blunted the release of PGI2 induced by ET-1 (50 nM). On the other hand, ET-2 was also able to trigger the release of PGI2 and to increase the perfusion pressure in this organ. The immediate precursor of ET-1, big ET-1 (0.5 microM), also induced a protracted increase in perfusion pressure. In contrast, big ET-2 (0.5 microM) was significantly weaker than big ET-1 in incr...Continue Reading

Citations

Sep 10, 2002·Journal of Hepatology·Paolo MontaltoAndrew K Burroughs
Feb 19, 1999·Lancet·J GoulisA K Burroughs
Jul 6, 2014·Therapeutic Advances in Cardiovascular Disease·Kazuya Miyagawa, Noriaki Emoto
Jul 19, 2001·The Journal of Veterinary Medical Science·R KamimuraK Miyahara

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