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Angiotensin II receptor antagonists
The Lancet, 2000 Blockade of the renin-angiotensin system began as a way of studying the pathogenesis of cardiovascular disease with specific pharmacological probes. Oral activity, achieved by shortening the original peptide structures, transformed the probes into therapeutic agents, the angiotensin-converting enzyme (ACE) inhibitors.
Burnier M, Brunner HR
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Angiotensin Receptors and Their Antagonists
New England Journal of Medicine, 1996Angiotensins are peptide hormones derived from the protein precursor angiotensinogen by the sequential actions of proteolytic enzymes (Figure 1). The classic pathway of angiotensin synthesis includes a reaction catalyzed by angiotensin-converting enzyme (ACE), which occurs not only in plasma but also in the kidneys, brain, adrenal glands, ovaries, and ...
T L, Goodfriend, M E, Elliott, K J, Catt
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Angiotensin II receptor antagonists and receptor subtypes
Trends in Endocrinology & Metabolism, 1992Recently discovered nonpeptide angiotensin II receptor antagonists represent a new class of potential drugs for the treatment of hypertension and congestive heart failure. Further, these antagonists have been successfully used as selective research tools for physiologic studies of angiotensin H and defining angiotensin II receptor subtypes.
P C, Wong +5 more
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Angiotensin II receptor antagonists and the kidney
Current Opinion in Nephrology and Hypertension, 1994The kidney is not only the source of circulating renin, which determines the plasma concentration of angiotensin II, but it is also one of the main targets of angiotensin II. Thus, angiotensin II exerts an important physiologic influence on renal function through its ability to modulate renal hemodynamics as well as glomerular and tubular functions ...
Burnier M, Brunner HR
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Angiotensin receptor antagonists
2014Abstract The renin–angiotensin–aldosterone system (RAAS) is activated in patients with heart failure and contributes to many of the detrimental effects seen in these patients. Antagonists to the angiotensin II type-1 (AT1)-receptor (ARBs) provide a pharmacologically different mechanism of inhibiting the RAAS to ACE inhibitors.
Roy S. Gardner +2 more
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Dihydropyrimidine angiotensin II receptor antagonists
Journal of Medicinal Chemistry, 1992The discovery of the nonpeptide angiotensin II (AII) receptor antagonist losartan, previously called DuP 753, has stimulated considerable interest in the synthesis of novel analogs of this compound. Our efforts in this area have resulted in the discovery of dihydropyrimidines as potent AII receptor antagonists. The chemistry leading to this novel class
K S, Atwal +9 more
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Overview of angiotensin II-receptor antagonists
The American Journal of Cardiology, 1998T renin–angiotensin system is integral to the mechanisms that regulate cardiovascular homeostasis. The renin–angiotensin system has an important role in the pathophysiology of hypertension and heart failure via the vasoconstricting effects of angiotensin II, which sustain elevated blood pressure levels in hypertension and increase afterload in chronic ...
B, Pitt, M A, Konstam
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Nonpeptide Angiotensin II Receptor Antagonists
American Journal of Hypertension, 1990Although the most direct way to interfere with the renin-angiotensin system (RAS) is at the level of the angiotensin II (AII) receptor, the currently available AII receptor antagonists are peptides still retaining significant agonistic properties with the obvious drawbacks of limited stability and lack of oral activity.
P B, Timmermans +8 more
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