Early-onset endothelin receptor blockade in hypertensive heterozygous Ren-2 rats.

Abstract	Male heterozygous Ren-2 transgenic rats and Hannover Sprague-Dawley rats fed a normal or high-salt diet were either untreated or treated with the nonselective receptor ET(A)/ET(B) receptor blocker bosentan or the selective ET(A) receptor blocker, ABT-627, known as atrasentan. Survival rate was partly increased by bosentan and fully normalized by atrasentan. Bosentan did not significantly influence the course of hypertension in TGR, whereas atrasentan significantly decreased BP on both diets. Atrasentan substantially reduced proteinuria, cardiac hypertrophy, glomerulosclerosis and left ventricular ET-1 tissue concentration on both diets. Our data indicate that ET(A) receptor blockade is superior to nonselective blockade in attenuating hypertension, end-organ damage and improving survival rate.
Authors	Ivana Vanecková, Herbert J Kramer, Angela Bäcker, Stanislava Schejbalová, Zdena Vernerová, Václav Eis, Martin Opocenský, Pavel Dvorák, Ludek Cervenka
Journal	Vascular pharmacology (Vascul Pharmacol) Vol. 45 Issue 3 Pg. 163-70 (Sep 2006) ISSN: 1537-1891 [Print] United States
PMID	16807127 (Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't)
Chemical References	Antihypertensive Agents Endothelin A Receptor Antagonists Endothelin B Receptor Antagonists Endothelin Receptor Antagonists Endothelin-1 Pyrrolidines Receptors, Endothelin Ren2 protein, mouse Sodium Chloride, Dietary Sulfonamides Renin Bosentan Atrasentan
Topics	Animals Animals, Genetically Modified Antihypertensive Agents (pharmacology, therapeutic use) Atrasentan Blood Pressure (drug effects) Body Weight (drug effects) Bosentan Cardiomegaly (prevention & control) Disease Models, Animal Endothelin A Receptor Antagonists Endothelin B Receptor Antagonists Endothelin Receptor Antagonists Endothelin-1 (metabolism) Glomerulosclerosis, Focal Segmental (prevention & control) Heterozygote Hypertension (chemically induced, metabolism, physiopathology, prevention & control) Male Proteinuria (prevention & control) Pyrrolidines (pharmacology, therapeutic use) Rats Rats, Sprague-Dawley Receptors, Endothelin (metabolism) Renin (genetics) Sodium Chloride, Dietary Sulfonamides (pharmacology, therapeutic use) Time Factors

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