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.
Full text
PDF
Selected References
These references are in PubMed. This may not be the complete list of references from this article.
- Arai H., Hori S., Aramori I., Ohkubo H., Nakanishi S. Cloning and expression of a cDNA encoding an endothelin receptor. Nature. 1990 Dec 20;348(6303):730–732. doi: 10.1038/348730a0. [DOI] [PubMed] [Google Scholar]
- D'Orléans-Juste P., Lidbury P. S., Telemaque S., Warner T. D., Vane J. R. Human big endothelin releases prostacyclin in vivo and in vitro through a phosphoramidon-sensitive conversion to endothelin-1. J Cardiovasc Pharmacol. 1991;17 (Suppl 7):S251–S255. doi: 10.1097/00005344-199100177-00072. [DOI] [PubMed] [Google Scholar]
- Fukuroda T., Noguchi K., Tsuchida S., Nishikibe M., Ikemoto F., Okada K., Yano M. Inhibition of biological actions of big endothelin-1 by phosphoramidon. Biochem Biophys Res Commun. 1990 Oct 30;172(2):390–395. doi: 10.1016/0006-291x(90)90685-g. [DOI] [PubMed] [Google Scholar]
- Ihara M., Fukuroda T., Saeki T., Nishikibe M., Kojiri K., Suda H., Yano M. An endothelin receptor (ETA) antagonist isolated from Streptomyces misakiensis. Biochem Biophys Res Commun. 1991 Jul 15;178(1):132–137. doi: 10.1016/0006-291x(91)91789-f. [DOI] [PubMed] [Google Scholar]
- Ihara M., Noguchi K., Saeki T., Fukuroda T., Tsuchida S., Kimura S., Fukami T., Ishikawa K., Nishikibe M., Yano M. Biological profiles of highly potent novel endothelin antagonists selective for the ETA receptor. Life Sci. 1992;50(4):247–255. doi: 10.1016/0024-3205(92)90331-i. [DOI] [PubMed] [Google Scholar]
- Sakurai T., Yanagisawa M., Takuwa Y., Miyazaki H., Kimura S., Goto K., Masaki T. Cloning of a cDNA encoding a non-isopeptide-selective subtype of the endothelin receptor. Nature. 1990 Dec 20;348(6303):732–735. doi: 10.1038/348732a0. [DOI] [PubMed] [Google Scholar]
- Salmon J. A. A radioimmunoassay for 6-keto-prostaglandin F1alpha. Prostaglandins. 1978 Mar;15(3):383–397. doi: 10.1016/0090-6980(78)90122-3. [DOI] [PubMed] [Google Scholar]
- Webb D. J. Endothelin receptors cloned, endothelin converting enzyme characterized and pathophysiological roles for endothelin proposed. Trends Pharmacol Sci. 1991 Feb;12(2):43–46. doi: 10.1016/0165-6147(91)90492-b. [DOI] [PubMed] [Google Scholar]
- de Nucci G., Thomas R., D'Orleans-Juste P., Antunes E., Walder C., Warner T. D., Vane J. R. Pressor effects of circulating endothelin are limited by its removal in the pulmonary circulation and by the release of prostacyclin and endothelium-derived relaxing factor. Proc Natl Acad Sci U S A. 1988 Dec;85(24):9797–9800. doi: 10.1073/pnas.85.24.9797. [DOI] [PMC free article] [PubMed] [Google Scholar]