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Endothelin receptor antagonists
Pharmacology & Therapeutics, 2006Endothelin receptor antagonists (ERAs) have been developed to block the effects of endothelin-1 (ET-1) in a variety of cardiovascular conditions. ET-1 is a powerful vasoconstrictor with mitogenic or co-mitogenic properties, which acts through the stimulation of 2 subtypes of receptors [endothelin receptor subtype A (ETA) and endothelin receptor subtype
Motte, Sophie +2 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.
Michael, Kirchengast, Matthias, Luz
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Diabetic Medicine, 2020
To analyse the efficacy and safety of endothelin receptor antagonists for people with diabetic kidney disease.
Y. Zhou +5 more
semanticscholar +1 more source
To analyse the efficacy and safety of endothelin receptor antagonists for people with diabetic kidney disease.
Y. Zhou +5 more
semanticscholar +1 more source
Transfer and Vascular Effect of Endothelin Receptor Antagonists in the Human Placenta
HYPERTENSION, 2019Supplemental Digital Content is available in the text. Increasing evidence suggests a role for the ET (endothelin) system in preeclampsia. Hence, blocking this system with endothelin receptor antagonists (ERAs) could be a therapeutic strategy.
E. Hitzerd +10 more
semanticscholar +1 more source
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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Endothelin Receptor Antagonists - An Overview
Current Medicinal Chemistry, 2002In thirteen years since the appearance of Endothelin (ET) on the international scene, possibility of its involvement in a variety of diseases has attracted the attention of medicinal chemists in search of novel therapeutics for various cardiovascular diseases (CVDs).
Falguni, Dasgupta +2 more
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Peptoids as endothelin receptor antagonists
Bioorganic & Medicinal Chemistry Letters, 2001A series of new peptoids as endothelin receptor antagonists has been synthesized. Screening them for their ability to bind with endothelin receptors (ET(A) and ET(B)) competitively in the presence of (125I) endothelin led to the discovery of compounds as possible leads with IC50s in the low micromolar concentrations.
F, Dasgupta +5 more
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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
Jia, Guo +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 ...
Josanna Rodriguez-Lopez +1 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.
Lewis J, Rubin, Sébastien, Roux
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