Use of A-192621 and IRL-2500 to unmask the mesenteric and renal vasodilator role of endothelin ET(B) receptors.

Journal of Cardiovascular Pharmacology
Susan Wai Sum LeungRicky Ying Keung Man

Abstract

Endothelin-1 (ET-1) is known to cause a transient (<1 min) depressor followed by a sustained (>1 h) pressor response. The former through the activation of ET(B) receptors, and the latter through the activation of ET(A) and ET(B) receptors. This study examines if ET(B) receptors mediate sustained mesenteric and renal dilation in anesthetized rats. Intravenous bolus ET-1 (0.8, 1.4, and 2 nmol/kg) and IRL-1620 (ET(B) agonist, 2, 5, and 10 nmol/kg) caused transient decrease followed by sustained increases in mean arterial pressure (MAP) that were accompanied by increases in total peripheral resistance (TPR), reductions in cardiac output (CO), and mesenteric and renal vasoconstriction. Pretreatment with FR-139317 (ET(A) antagonist, 1 mg/kg) attenuated the pressor and constrictor effects of ET-1 but did not alter responses to IRL-1620. IRL-2500 (ET(B) antagonist, 5 mg/kg) slightly inhibited the renal constrictor effect of IRL-1620, whereas A-192621 (ET(B) antagonist, 5 mg/kg) abolished all hemodynamic responses to IRL-1620. Both IRL-2500 and A-192621 markedly enhanced MAP, TPR, and mesenteric, and the renal constrictor effects of ET-1. Therefore, A-192621 was more effective than IRL-2500 in blocking IRL-1620-induced vasoconstriction,...Continue Reading

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Citations

Aug 13, 2003·Hypertension·Hugo C D SouzaMaria Cristina O Salgado
Dec 18, 2003·American Journal of Physiology. Renal Physiology·Armin JustWilliam J Arendshorst
Feb 7, 2003·American Journal of Physiology. Gastrointestinal and Liver Physiology·C E King-VanVlackP H MacDonald
Dec 25, 2004·American Journal of Physiology. Regulatory, Integrative and Comparative Physiology·Armin JustWilliam J Arendshorst
Apr 10, 2012·Biochemical Pharmacology·Marc Q Mazzuca, Raouf A Khalil

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