Results 191 to 200 of about 15,820 (232)
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Enrasentan, an Antagonist of Endothelin Receptors
Cardiovascular Drug Reviews, 2003ABSTRACTEndothelins are powerful vasoconstrictor agents produced by endothelial cells and identified by Yanagisawa et al. in 1988. Two types of receptors for endothelins have been identified: ETAreceptors are located on smooth muscle cells of the vascular wall and are responsible for endothelin‐induced vasoconstriction while ETBreceptors are located on
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Endothelin and Endothelin Receptor Antagonists in Heart Failure
Congestive Heart Failure, 2002Endothelin (ET) is a recently discovered 21‐amino acid peptide that has potent physiologic and pathophysiologic effects that appear to be involved in the development of heart failure. These include effects on arterial smooth muscle cells that cause intense peripheral vasoconstriction and stimulation of cardiac myocytes and fibroblasts.
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Endothelin Receptors and Receptor Antagonists
1998Multiple receptor subtypes for endothelin have been identified in pharmacological studies both in vitro and in vivo. As can be evidenced in the study by Yanagisawa et al, at least two receptor subtypes may be responsible for the biphasic nature of the hemodynamic response to intravenous injection of ET-1: a transient hypotension followed by a sustained
Andrew S. Tasker, David M. Pollock
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Role of endothelin and endothelin receptor antagonists in renal disease
European Journal of Clinical Investigation, 2006AbstractEndothelin (ET)‐1 is a potent vasoconstrictor peptide with pro‐inflammatory, mitogenic, and pro‐fibrotic properties that is closely involved in both normal renal physiology and pathology. ET‐1 exerts a wide variety of biological effects, including constriction of cortical and medullary vessels, mesangial cell contraction, stimulation of ...
W, Neuhofer, D, Pittrow
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Endothelins and endothelin receptor antagonists: Binding to plasma proteins
Life Sciences, 1996Endothelins (ET) are 21-amino acid peptides that bind to membrane receptors to initiate a wide range of pathophysiological effects. PD-156707, L-749329, Ro-470203, and A-127722 are potent non-peptide ET receptor antagonists developed recently. When tested in human and rat plasma, both ET-1 and -3 and the four aforementioned antagonists exhibited a high
J R, Wu-Wong +5 more
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Endothelin Receptor Antagonists
2015Endothelin-1 (ET-1) is a potent vasoconstrictor and mitogen that is secreted by the endothelium. Pulmonary vascular expression of endothelin is increased in pulmonary hypertension and plasma levels correlate with the severity of disease. Several endothelin receptor antagonists (ERAs) have been developed and are available for the treatment of pulmonary ...
Josanna Rodriguez-Lopez +1 more
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Endothelin-Receptor Antagonists in Uremic Cardiomyopathy
Journal of Cardiovascular Pharmacology, 2000Increased endothelin-1 (ET-1) levels were found in patients with chronic renal failure. These correlate with the severity of renal failure. Patients with elevated ET-1 concentrations show an increased cardiovascular mortality. The prevalence of severe left ventricular hypertrophy (LVH) is a very important factor for survival and morbidity in uremic ...
S C, Wolf +6 more
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[Endothelin receptor antagonist].
Nihon rinsho. Japanese journal of clinical medicine, 2009Pulmonary arterial hypertension(PAH) is an uncommon disease characterised by a progressive increase in pulmonary vascular resistance. An imbalance between vasoconstrictor/vasodilator activities could be responsible for altered pulmonary vascular tone and structure. In PAH patients, endothelin are increased.
Takuya, Kishi, Kenji, Sunagawa
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Heart failure and endothelin receptor antagonists
Trends in Pharmacological Sciences, 1999Cardiac myocytes and vascular endothelial cells produce endothelin-1, which increases the contractility of cardiac muscles and of vascular smooth muscles. Endothelin-1 also exerts long-term effects, such as myocardial hypertrophy, and causes cellular injury in cardiac myocytes.
T, Miyauchi, K, Goto
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Bis-sulfonamides as endothelin receptor antagonists
Bioorganic & Medicinal Chemistry Letters, 2003Modification of the structure of bosentan 1, the first marketed endothelin receptor antagonist (Tracleer), by introduction of a second sulfonamide function at the alkoxy side chain, led to bis-sulfonamides 2. This allowed to prepare dual ET(A)/ET(B) as well as ET(B) receptor selective antagonists, which could serve as tools to investigate the ...
Christoph, Boss +4 more
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