PMID: 8587398Jan 1, 1995Paper

Delineation of endothelin receptor subtypes in rat and rabbit aortas

Journal of Cardiovascular Pharmacology
S S ShettyA Y Jeng

Abstract

The receptor subtypes mediating tension responses to endothelin-1 (ET-1) in isolated rat and rabbit aortic preparations were examined with various ET receptor antagonists. In the presence of 3 microM IRL 2500 (an ETB-selective antagonist), SB 209670 (an ETA/ETB antagonist) induced monophasic inhibitions of the ET-1 dose-response curves of both rat (pKB 9.1) and rabbit aortas (pKB 8.9). In the presence of IRL 2500, PD 156707 (an ETA antagonist) also caused a similar monophasic inhibition of the agonist-induced dose-response curve of the rat aorta (pKB 7.7) but produced a biphasic inhibition of the curve obtained with the rabbit aorta. PD 156707, however, produced monophasic inhibitions of the ET-1-induced dose-response curve of rabbit aortas pretreated either with BQ 788 (an ETB-selective antagonist) or desensitized with sarafotoxin S6c (an ETB-selective agonist). The receptor subtypes mediating the contractile responses to ET-1 were further characterized by examining the effects of the antagonists on the binding of [125I]ET-1 to these two tissues. In the presence of 1 nM IRL 2500, SB 209670 displaced [125I]ET-1 binding in both rat and rabbit aortic membrane preparations in a monophasic manner, with similar potencies (IC50 1.2-1...Continue Reading

Citations

Aug 23, 2001·Pharmacology & Therapeutics·P W Hadoke
Apr 25, 2006·British Journal of Pharmacology·Carlos R TirapelliPedro D'Orleans-Juste
Jun 12, 2002·Canadian Journal of Physiology and Pharmacology·Gary M KsanderArco Y Jeng

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