Results 261 to 270 of about 18,452 (302)
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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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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 ...
Martin Bolli +4 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 ...
Richard N. Channick +1 more
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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 Receptor Antagonist
2017Endothelin (ET)-1, a peptide mainly produced by vascular endothelial cells, has potent and long-lasting vasoconstrictive effect. In addition, ET-1 has been shown to induce a variety of biological effects including cell proliferation, inflammation, and fibrosis.
Noriaki Emoto, Noriaki Emoto
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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
David M. Pollock, Andrew S. Tasker
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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.
Katsutoshi Goto, Takashi Miyauchi
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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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The renoprotective potential of endothelin receptor antagonists
Expert Opinion on Investigational Drugs, 2000The 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 +5 more
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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
Jinshyun R. Wu-Wong +5 more
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