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Endothelin receptor antagonists: a brief review [PDF]

Canadian Journal of Physiology and Pharmacology, 1994
The endothelins are a family of potent vasoconstrictors, some of which also have vasodilatory activity. In many diseases associated with tissue hypoxia or ischemia and in diseases in which vasoconstriction plays a role, the circulating levels of endothelin are higher than in healthy, control subjects.
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Endothelin Receptors and Receptor Antagonists

1998
Multiple 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
David M. Pollock, Andrew S. Tasker
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Heart failure and endothelin receptor antagonists

Trends in Pharmacological Sciences, 1999
Cardiac 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.
Katsutoshi Goto, Takashi Miyauchi
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Sildenafil versus Endothelin Receptor Antagonist for Pulmonary Hypertension (SERAPH) study.

American Journal of Respiratory and Critical Care Medicine, 2005
RATIONALE Phosphodiesterase type 5 (PDE5) inhibition has been proposed for the treatment for pulmonary arterial hypertension (PAH). OBJECTIVE This study compared adding sildenafil, a PDE5 inhibitor, to conventional treatment with the current practice ...
M. Wilkins, G. Paul, J. Strange, N. Tunariu, W. Gin-Sing, W. Banya, M. Westwood, A. Stefanidis, L. Ng, D. Pennell, R. Mohiaddin, P. Nihoyannopoulos, J. Gibbs   +12 more
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Endothelin and Endothelin Receptor Antagonists in Heart Failure

Congestive Heart Failure, 2002
Endothelin (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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The renoprotective potential of endothelin receptor antagonists

Expert Opinion on Investigational Drugs, 2000
The endothelin system has been identified as having a substantial role in renal failure, both acute and chronic. Beside its well characterised haemodynamic effects, its mitogenic and pro-fibrotic properties have gained increased interest in the pathophysiology of chronic renal failure.
Peter Rohmeiss, Claude Braun, K.P. Juenemann, Rainer Birck, Thomas Knoll, M. Schaub   +5 more
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Endothelins and endothelin receptor antagonists: Binding to plasma proteins

Life Sciences, 1996
Endothelins (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
Jinshyun R. Wu-Wong, Daniel J. Huffman, William J. Chiou, Martin Winn, Terry J. Opgenorth, Thomas W. von Geldern   +5 more
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Role of endothelin and endothelin receptor antagonists in renal disease

European Journal of Clinical Investigation, 2006
AbstractEndothelin (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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An endothelin receptor antagonist TAK-044 ameliorates carbon tetrachloride-induced acute liver injury and portal hypertension in rats.

Liver, 2008
Hepatic levels of a powerful vasoconstrictor endothelin-1 (ET-1) and its receptors increase in human and carbon tetrachloride (CCl4)-induced liver cirrhosis.
C. Gandhi, E. Nemoto, Simon C Watkins, V. Subbotin   +3 more
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Endothelin Receptor Antagonists in Cancer Therapy

Cancer Investigation, 2007
Endothelins are a family of peptide compounds which exert regulatory control over cellular processes important for growth, survival, invasion, and angiogenesis. In particular, endothelin-1, acting primarily through the endothelin-A receptor, is implicated in the neoplastic growth of multiple tumor types.
George Wilding, Mihailo Lalich, Glenn Liu, Douglas G. McNeel   +3 more
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