Document Detail


Prolonged anti-hypertensive effects of oral sitaxsentan, a selective ET(A) endothelin receptor antagonist, in spontaneoulsy hypertensive hamsters.
MedLine Citation:
PMID:  17043751     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
INTRODUCTION: The purpose of this study was to determine whether prolonged oral therapy with sitaxsentan, a potent selective ET(A) endothelin receptor antagonist, normalizes systolic blood pressure in spontaneously hypertensive hamsters, a new rodent model of high-renin genetic hypertension. MATERIALS AND METHODS: Spontaneously hypertensive hamsters received either oral sitaxsentan (15 mg kg(-1) day(-1)) dissolved in high purity water or saline for 7 weeks. Systolic blood pressure was monitored in lightly anesthetized animals using the leg-cuff method. RESULTS: We found that sitaxsentan elicited a significant decrease in systolic blood pressure in spontaneously hypertensive hamsters from 175 +/- 6 mmHg at baseline to 109 +/- 7 mmHg after 7 weeks (p < 0.05). Although treatment of spontaneously hypertensive hamsters with saline was also associated with a significant decrease in systolic blood pressure from baseline, the magnitude of response was significantly less than that observed with sitaxsentan (p < 0.05). DISCUSSION: Collectively, these proof-of-principle data indicate that prolonged oral sitaxsentan therapy normalizes systolic blood pressure in spontaneously hypertensive hamsters. We suggest that selective ET(A) endothelin receptor blockade could be beneficial in the treatment of essential hypertension associated with high renin plasma levels.
Authors:
Israel Rubinstein
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Cardiovascular drugs and therapy / sponsored by the International Society of Cardiovascular Pharmacotherapy     Volume:  20     ISSN:  0920-3206     ISO Abbreviation:  Cardiovasc Drugs Ther     Publication Date:  2006 Oct 
Date Detail:
Created Date:  2006-12-12     Completed Date:  2007-05-18     Revised Date:  2008-06-05    
Medline Journal Info:
Nlm Unique ID:  8712220     Medline TA:  Cardiovasc Drugs Ther     Country:  United States    
Other Details:
Languages:  eng     Pagination:  387-90     Citation Subset:  IM    
Affiliation:
Departments of Medicine and Biopharmaceutical Sciences, Colleges of Medicine and Pharmacy, University of Illinois at Chicago, Chicago, IL 60612, USA. IRubinst@uic.edu
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MeSH Terms
Descriptor/Qualifier:
Animals
Antihypertensive Agents / pharmacology*
Blood Pressure / drug effects
Cricetinae
Hypertension / drug therapy*,  physiopathology
Isoxazoles / pharmacology*
Male
Receptor, Endothelin A / antagonists & inhibitors*
Thiophenes / pharmacology*
Chemical
Reg. No./Substance:
0/Antihypertensive Agents; 0/Isoxazoles; 0/Receptor, Endothelin A; 0/Thiophenes; 0/sitaxsentan

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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