Results 51 to 60 of about 304,614 (388)

The discovery of N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propylsulfamide (Macitentan), an orally active, potent dual endothelin receptor antagonist.

Journal of Medicinal Chemistry, 2012
Starting from the structure of bosentan (1), we embarked on a medicinal chemistry program aiming at the identification of novel potent dual endothelin receptor antagonists with high oral efficacy.
M. Bolli, C. Boss, C. Binkert, Stephan Buchmann, D. Bur, P. Hess, M. Iglarz, Solange Meyer, J. Rein, Markus Rey, A. Treiber, M. Clozel, W. Fischli, T. Weller   +13 more
semanticscholar   +1 more source

Anti-adrenergic effects of endothelin on human atrial action potentials are potentially anti-arrhythmic [PDF]

, 2006
Endothelin-1 (ET-1) is elevated in patients with atrial fibrillation (AF) and heart failure. We investigated effects of ET-1 on human atrial cellular electrophysiological measurements expected to influence the genesis and maintenance of AF.
Kane, K.A., Rankin, A.C., Redpath, C., Workman, A.J.   +3 more
core   +1 more source

Digital ulcers in systemic sclerosis: prevention by treatment with bosentan, an oral endothelin receptor antagonist.

Arthritis & Rheumatism, 2004
OBJECTIVE Recurrent digital ulcers are a manifestation of vascular disease in patients with systemic sclerosis (SSc; scleroderma) and lead to pain, impaired function, and tissue loss.
J. Korn, M. Mayes, M. Cerinic, M. Rainisio, J. Pope, E. Hachulla, É. Rich, P. Carpentier, J. Molitor, J. Seibold, V. Hsu, L. Guillevin, Sharmila Chatterjee, H. Peter, J. Coppock, A. Herrick, P. Merkel, R. Simms, C. Denton, D. Furst, N. Nguyen, M. Gaitonde, C. Black   +22 more
semanticscholar   +1 more source

Direct angiotensin AT2 receptor stimulation using a novel AT2 receptor agonist, compound 21, evokes neuroprotection in conscious hypertensive rats [PDF]

, 2014
Background: In this study, the neuroprotective effect of a novel nonpeptide AT2R agonist, C21, was examined in a conscious model of stroke to verify a class effect of AT2R agonists as neuroprotective agents.
Alterman, Mathias, Callaway, Jennifer K., Hallberg, Anders, McCarthy, Claudia A., Miller, Alyson A., Vinh, Antony, Widdop, Robert E.   +6 more
core   +2 more sources

Interleukin-2 receptor antagonists for pediatric liver transplant recipients: A systematic review and meta-analysis of controlled studies [PDF]

Pediatric Transplantation, 18(8):839-850, 2014, 2014
Interleukin-2 receptor antagonists (IL-2RA) are frequently used as induction therapy in liver transplant recipients to decrease the risk of acute rejection while allowing the reduction of concomitant immunosuppression. The exact association with the use of IL-2RA however is uncertain.
arxiv   +1 more source

VIP and endothelin receptor antagonist: An effective combination against experimental pulmonary arterial hypertension

Respiratory Research, 2011
BackgroundPulmonary Arterial Hypertension (PAH) remains a therapeutic challenge, and the search continues for more effective drugs and drug combinations.
S. Hamidi, R. Lin, A. Szema, S. Lyubsky, Yaping Jiang, S. Said   +5 more
semanticscholar   +1 more source

Kinetics of endothelin-1 and effect selective ET_A antagonism on ET_B activation: a mathematical modeling analysis. [PDF]

Front Pharmacol
IntroductionEndothelin-1 (ET-1) regulates renal and vascular function, but the clinical utility of selective ETA receptor antagonists has been limited due to associated fluid retention.
Hallow KM, Greasley PJ, Heerspink HJL, Yu H.   +3 more
europepmc   +2 more sources

Comparison of the structures of the endothelin A receptor antagonists BQ123 and N-methyl leucine BQ123 with the crystal structure of the C-terminal tail of endothelin-1 [PDF]

The functionally important regions of the cyclic pentapeptide endothelin A receptor antagonist BQ123 are shown to correlate with the structure of the C-terminal tail of endothelin-1, as found in the recently-determined X-ray crystal structure.
Janes, Robert W., Peishoff, Catherine E., Wallace, B.A.   +2 more
core   +1 more source

Baseline characteristics and enrichment results from the SONAR trial [PDF]

, 2018
Aim: The SONAR trial uses an enrichment design based on the individual response to the selective endothelin receptor antagonist atrasentan on efficacy (the degree of the individual response in the urinary albumin‐to‐creatinine ratio [UACR]) and safety/
Andress, Dennis L., Bakris, George, Brennan, John J., Correa-Rotter, Ricardo, de Zeeuw, Dick, Heerspink, Hiddo J.L., Hou, Fan Fan, Kitzman, Dalane W., Kohan, Donald, Makino, Hirofumi, McMurray, John, Parving, Hans-Henrik, Perkovic, Vlado, Tobe, Sheldon, Wigderson, Melissa, Yi, Tingting   +15 more
core   +3 more sources

Bioengineering a Patient‐Derived Vascularized Lung Tumor‐on‐Chip Model to Decipher Immunomodulation by the Endothelium

Advanced Healthcare Materials, EarlyView.
Most in vitro cancer models lack cellular diversity, functional complexity, and clinical relevance. This work highlights the generation of an innovative dynamic tetraculture with autologous patient‐derived cells within a vascularized tumor‐on‐chip, as well as the recapitulation of endothelial anergy features induced by the tumor microenvironment ...
Christine Lansche, Ségolène Ladaigue, Giacomo Gropplero, Nicolas Zimmermann, Martin Nurmik, Irina Veith, Manh‐Louis Nguyen, Solenn Brosseau, Nicolas Poté, Pierre Mordant, Arnaud Roussel, Fathia Mami‐Chouaib, Fatima Mechta‐Grigoriou, Gérard Zalcman, Fabrice Soncin, Stéphanie Descroix, Maria Carla Parrini   +16 more
wiley   +1 more source