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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
2013Three pathways have been identified in the pathogenesis of pulmonary arterial hypertension (PAH): the endothelin (ET), nitric oxide (NO) and prostacyclin pathways. These pathways represent the targets of approved PAH therapies and their discovery has facilitated significant progress in the understanding and treatment of PAH.
Martine, Clozel +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.
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The endothelin system and endothelin receptor antagonists
Current Opinion in Nephrology & Hypertension, 2012There is increasing evidence that endothelin receptor blockade and, in particular, ET(A) receptor blockade not only confers protection against proteinuric renal disease in diabetes but also confers vasculoprotection.Recent clinical trials using ET(A) receptor blockade in treating proteinuria and chronic kidney disease as well as atherosclerosis show ...
Karin A M, Jandeleit-Dahm +1 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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Heterogeneity of Endothelin Receptor
Journal of Cardiovascular Pharmacology, 1991The complex formed between endothelin (ET) and its binding protein was adequately stable to be separated by sodium dodecyl sulfate (SDS)-polyacrylamide gel electrophoresis (PAGE) at low temperature. Cross-linking was not necessary. This simple method was applied for both qualitative (determination of molecular weight of ET binding protein) and ...
T, Takasuka +4 more
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Endothelin Receptor Antagonism
1995Following the original report by Yanagisawa et al. (1988) more than 7 years ago, compelling evidence that ET plays an important role in the local regulation of smooth muscle tone and cell growth has been reported. In addition, many studies point to a significant role for endothelin in nonvascular function. The investigation of the endothelin system has
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Endothelin and Endothelin Receptor Antagonism in Heart Failure
Journal of Cardiovascular Pharmacology, 2000Endothelin (ET)-1 is a potent vasoconstrictor with growth promoting and mitogenic properties associated with various cardiovascular diseases (CVD) and has been found to be an important protagonist in congestive heart failure (CHF). The introduction of ET-1 receptor antagonists into the arena of clinical research has amplified our understanding of the ...
G, Sütsch, W, Kiowski
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Endothelin and endothelin receptor antagonism in portopulmonary hypertension
European Journal of Clinical Investigation, 2006AbstractPortopulmonary hypertension (PPHT) is a rare but devastating complication in patients with portal hypertension, characterized by pulmonary arterial obliterative disease with a concomitant rise in pulmonary vascular resistance. A broad body of evidence has accumulated, indicating that endothelin (ET) peptides and their cognate receptors are ...
W, Neuhofer, V, Gülberg, A L, Gerbes
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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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