PMID: 8587352Jan 1, 1995Paper

Pharmacologic evidence for the presence of three functional endothelin receptor subtypes in rabbit saphenous vein

Journal of Cardiovascular Pharmacology
S A DouglasE Ohlstein

Abstract

The contractile responses to endothelin-1 (ET-1), endothelin-3 (ET-3), and sarafotoxin S6c (STXc) were best-fitted by a two-site model in the rabbit isolated saphenous vein. Agonists were equipotent at the high-affinity site (pD2s 12.0 +/- 0.2, 12.2 +/- 0.2, and 12.3 +/- 0.3, respectively), characteristic of an ETB receptor, whereas ET-3 and STXc were significantly more potent than ET-1 as vasoconstrictors at the low-affinity site (pD2s 10.2 +/- 0.3, 10.6 +/- 0.3, and 9.1 +/- 0.1, respectively), characteristic of an ETC-like receptor. The high affinity, ETB-mediated response was inhibited by SB 209670, Ro 47-0203, BQ-788, and Ro 46-2005 (Kbs of 0.15, 14, 110, and 280 nM against STXc, respectively) but was insensitive to PD 142893, RES-701 and BQ-123 (Kbs > or = 10 microM), consistent with this response being mediated by the ETB2-like receptor subtype. The low-affinity ETC-like-mediated component was inhibited by SB 209670, Ro 47-0203, BQ-788, Ro 46-2005, PD 142893, and RES-701 (Kbs 38 nM, 62 nM, 670 nM, 580 nM, 1.7 microM, and 2.0 microM, respectively), but was insensitive to BQ-123 (Kb > or = 10 microM). ET-3 produced endothelium-dependent vasorelaxation in the presence of active tone. Antagonist IC50s were approximated as bei...Continue Reading

Citations

Apr 6, 2004·Trends in Pharmacological Sciences·Tomoh Masaki
Aug 12, 1999·European Journal of Pharmacology·T MasakiY Okamoto
Jun 16, 2010·Pharmacology & Therapeutics·Cang-Bao XuLars Edvinsson
Oct 19, 2006·Comparative Biochemistry and Physiology. Part A, Molecular & Integrative Physiology·Maria Cristina BrenoNorma Yamanouye
Jul 26, 2002·Journal of Glaucoma·Thomas YorioGanesh Prasanna

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