Abstract
The ETA receptor antagonist, BQ-123 (1 microM) potently antagonized endothelin-1 (ET-1) concentration-response curves in guinea-pig aorta (pKB = 7.1). However, 10 microM BQ-123 was without effect on ET-1-induced contractions in guinea-pig bronchus. The ETB-selective agonist, sarafotoxin S6c did not contract the aorta but was a potent and effective contractile agonist in the bronchus. BQ-123 (10 microM) was without effect on sarafotoxin S6c-induced contractions in the bronchus. These data provide evidence for distinct endothelin receptors in guinea-pig aorta and bronchus, which appear to be predominantly of the ETA and non-ETA, perhaps ETB, subtypes, respectively.
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Selected References
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- 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]
- Cardell L. O., Uddman R., Edvinsson L. Evidence for multiple endothelin receptors in the guinea-pig pulmonary artery and trachea. Br J Pharmacol. 1992 Feb;105(2):376–380. doi: 10.1111/j.1476-5381.1992.tb14261.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Harrison V. J., Randriantsoa A., Schoeffter P. Heterogeneity of endothelin-sarafotoxin receptors mediating contraction of pig coronary artery. Br J Pharmacol. 1992 Mar;105(3):511–513. doi: 10.1111/j.1476-5381.1992.tb09009.x. [DOI] [PMC free article] [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]
- Maggi C. A., Giuliani S., Patacchini R., Santicioli P., Rovero P., Giachetti A., Meli A. The C-terminal hexapeptide, endothelin-(16-21), discriminates between different endothelin receptors. Eur J Pharmacol. 1989 Jul 4;166(1):121–122. doi: 10.1016/0014-2999(89)90693-6. [DOI] [PubMed] [Google Scholar]
- Masuda Y., Miyazaki H., Kondoh M., Watanabe H., Yanagisawa M., Masaki T., Murakami K. Two different forms of endothelin receptors in rat lung. FEBS Lett. 1989 Nov 6;257(2):208–210. doi: 10.1016/0014-5793(89)81535-2. [DOI] [PubMed] [Google Scholar]
- Sakamoto A., Yanagisawa M., Sakurai T., Takuwa Y., Yanagisawa H., Masaki T. Cloning and functional expression of human cDNA for the ETB endothelin receptor. Biochem Biophys Res Commun. 1991 Jul 31;178(2):656–663. doi: 10.1016/0006-291x(91)90158-4. [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]
- Williams D. L., Jr, Jones K. L., Pettibone D. J., Lis E. V., Clineschmidt B. V. Sarafotoxin S6c: an agonist which distinguishes between endothelin receptor subtypes. Biochem Biophys Res Commun. 1991 Mar 15;175(2):556–561. doi: 10.1016/0006-291x(91)91601-8. [DOI] [PubMed] [Google Scholar]
- Yanagisawa M., Masaki T. Endothelin, a novel endothelium-derived peptide. Pharmacological activities, regulation and possible roles in cardiovascular control. Biochem Pharmacol. 1989 Jun 15;38(12):1877–1883. doi: 10.1016/0006-2952(89)90484-x. [DOI] [PubMed] [Google Scholar]