Randomized Dose-Response Study of the New Dual Endothelin Receptor Antagonist Aprocitentan in Hypertension. [PDF]
Supplemental Digital Content is available in the text. This study examined the dose-response characteristics of aprocitentan, a dual endothelin A/endothelin B receptor antagonist, in patients with essential hypertension.
Verweij P +4 more
europepmc +2 more sources
The Selective Endothelin Receptor Antagonist SC0062 in IgA Nephropathy: A Randomized Double-Blind Placebo-Controlled Clinical Trial. [PDF]
Visual Abstract Key Points Patients with IgA nephropathy and significant proteinuria are at high risk of progressive kidney function loss and kidney failure. We report the results of a clinical trial assessing the selective endothelin receptor antagonist
Heerspink HJL +22 more
europepmc +2 more sources
Clinical pharmacokinetics and pharmacodynamics of the endothelin receptor antagonist macitentan. [PDF]
Pulmonary arterial hypertension (PAH) is a progressive disease of the lung vascular system, which leads to right-sided heart failure and ultimately death if untreated. Treatments to regulate the pulmonary vascular pressure target the prostacyclin, nitric
Sidharta PN, Treiber A, Dingemanse J.
europepmc +2 more sources
The diuretic effects achieved with sodium glucose co-transporter 2 inhibitors (SGLT2i) may offset fluid retaining effects of the endothelin receptor antagonist (ERA) atrasentan while effects on albuminuria and kidney protection of both drug classes may ...
H. Heerspink, D. Kohan, D. de Zeeuw
semanticscholar +1 more source
Slow receptor dissociation kinetics differentiate macitentan from other endothelin receptor antagonists in pulmonary arterial smooth muscle cells. [PDF]
Two endothelin receptor antagonists (ERAs), bosentan and ambrisentan, are currently approved for the treatment of pulmonary arterial hypertension (PAH), a devastating disease involving an activated endothelin system and aberrant contraction and ...
John Gatfield +4 more
doaj +1 more source
Endothelin Receptors and Their Antagonists
All three members of the endothelin (ET) family of peptides, ET-1, ET-2, and ET-3, are expressed in the human kidney, with ET-1 being the predominant isoform. ET-1 and ET-2 bind to two G-protein-coupled receptors, ETA and ETB, whereas at physiological concentrations ET-3 has little affinity for the ET(A) receptor.
Maguire, Janet J, Davenport, Anthony P
openaire +3 more sources
Background: Nicotinamide adenine dinucleotide phosphate (NADPH) oxidase (Nox) is one of the predominant sources of the production of free oxygen radicals in the vascular wall.
Parisa Dayati +3 more
doaj +1 more source
Therapeutic efficacy of TBC3711 in monocrotaline-induced pulmonary hypertension
Background Endothelin-1 signalling plays an important role in pathogenesis of pulmonary hypertension. Although different endothelin-A receptor antagonists are developed, a novel therapeutic option to cure the disease is still needed.
Brandes Ralf P +13 more
doaj +1 more source
Limited evidence is available on outcomes associated with currently available medications from the endothelin receptor antagonist drug class (bosentan, ambrisentan, and macitentan) in elderly patients with pulmonary arterial hypertension.
Raymond L. Benza +6 more
doaj +1 more source
EGF Receptor Transactivation by Endothelin-1 Increased CHSY-1 Mediated by NADPH Oxidase and Phosphorylation of ERK1/2 [PDF]
Objective: Growth factors [transforming growth factor-β (TGF-β), epidermal growth factor (EGF), endothelin-1 (ET-1)] stimulate proteoglycan synthesis resulting in retention and accumulation of low density lipoprotein (LDL) in vessel intima and leading to
Hossein Babaahmadi-Rezaei +5 more
doaj +1 more source

