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Endothelin Receptor Antagonists [PDF]
Pharmacology & Therapeutics, 2006 Endothelin 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
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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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Biotinylated endothelin as a probe for the endothelin receptor
Peptides, 1991Biotinylated derivatives of endothelin (ET)-1 were prepared by chemical modification of ET-1 with sulfosuccinimidyl 6-(biotinamido) hexanoate. Two major biotinylated ET analogs were purified by reversed-phase high performance liquid chromatography.
I, Schvartz +4 more
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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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Development of a Photolabile Ligand for the Endothelin-A Receptor of Endothelin
Journal of Cardiovascular Pharmacology, 2000Actions of endothelin (ET) are usually mediated through the so-called endothelin-A or -B (ET(A) or ET(B))-receptors. As part of our ongoing research program, we are studying the characterization of the ET(A)-receptor using specific photolabile ligands.
S, Tessier +5 more
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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, 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 and endothelin receptors A and B in the human testis
Anatomy and Embryology, 1999Human testicular capillaries interconnect Leydig cells and seminiferous tubules. Microcirculation and blood flow are therefore essential for the maintenance of spermatogenesis. The expression and the localisation of ET (endothelin) and its receptors in testicular tissue, in seminiferous tubules and in human testicular capillaries were studied.
S, Ergün +4 more
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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 ...
Sütsch G, Kiowski W
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