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Endothelin receptor antagonist for subarachnoid haemorrhage
Cochrane Database of Systematic Reviews, 2010A subarachnoid hemorrhage (SAH) is a serious and potentially life-threatening condition where blood leaks out of blood vessels over the surface of the brain. Delayed ischemic neurological deficit (DIND) and the related feature of vasospasm, where patients experience a delayed deterioration, have long been recognized as the leading potentially treatable
Lei Jiang +4 more
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Endothelin receptor antagonists
World Journal of Urology, 2005Hormone refractory prostate cancer remains true to its middle name: it is largely refractory to attempts to delay its progression. New targets and new therapies are demanded. Through a review of the available literature on endothelin and several preclinical observations, the endothelin axis has emerged as one such target.
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Thiophenesulfonamides as endothelin receptor antagonists
Bioorganic & Medicinal Chemistry Letters, 1996AbstractChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Adam Kois +6 more
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Endothelin, endothelin receptors, and endothelin antagonists
Current Opinion in Nephrology and Hypertension, 1994Endothelin is a peptide with potent biologic effects in vascular and nonvascular cells. Its effects are mediated by two receptors, ETA and ETB, and possibly also by a third receptor, ETC. In vascular smooth muscle cells, endothelin causes profound contraction and also has proliferative effects, mainly through activation of ETA but also through ETB ...
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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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Bosentan: a dual endothelin receptor antagonist
Expert Opinion on Investigational Drugs, 2002The peptide endothelin plays a significant role in a wide array of pathological conditions, including primary pulmonary hypertension and pulmonary arterial hypertension associated with collagen vascular disease. These are life-threatening conditions that can severely compromise the function of the lungs and heart.
Sébastien Roux, Lewis J. Rubin
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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 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 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 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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