scholarly journals The Discovery ofN-[5-(4-Bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N′-propylsulfamide (Macitentan), an Orally Active, Potent Dual Endothelin Receptor Antagonist

2012 ◽  
Vol 55 (17) ◽  
pp. 7849-7861 ◽  
Author(s):  
Martin H. Bolli ◽  
Christoph Boss ◽  
Christoph Binkert ◽  
Stephan Buchmann ◽  
Daniel Bur ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Endothelin Receptor Antagonist ◽  
Endothelin Receptor ◽  
Orally Active

Pharmacological Characterization of PABSA, an Orally Active and Highly Potent Endothelin-Receptor Antagonist

1999 ◽  
Vol 34 (1) ◽  
pp. 139-147 ◽  
Author(s):  
Takanori Iwasaki ◽  
Shin-ichi Mihara ◽  
Toshitake Shimamura ◽  
Masaru Kawakami ◽  
Yoko Hayasaki-Kajiwara ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Endothelin Receptor Antagonist ◽  
Endothelin Receptor ◽  
Pharmacological Characterization ◽  
Orally Active

Orally Active Endothelin Receptor Antagonist BMS-182874 Suppresses Neointimal Development in Balloon-Injured Rat Carotid Arteries

1995 ◽  
Vol 26 (6) ◽  
pp. 908-915 ◽  
Author(s):  
Patricia Ferrer ◽  
Maria Valentine ◽  
Tonya Jenkins-West ◽  
Helen Weber ◽  
Nancy L. Goller ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Carotid Arteries ◽  
Endothelin Receptor Antagonist ◽  
Endothelin Receptor ◽  
Orally Active

Pharmacology of Macitentan, an Orally Active Tissue-Targeting Dual Endothelin Receptor Antagonist

2008 ◽  
Vol 327 (3) ◽  
pp. 736-745 ◽  
Author(s):  
Marc Iglarz ◽  
Christoph Binkert ◽  
Keith Morrison ◽  
Walter Fischli ◽  
John Gatfield ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Endothelin Receptor Antagonist ◽  
Endothelin Receptor ◽  
Tissue Targeting ◽  
Orally Active

scholarly journals BOSENTAN - endothelin receptor antagonist

2018 ◽  
Vol 3 (1) ◽  
pp. 10
Author(s):  
Kiran Kumar Singal ◽  
Neerja Singal ◽  
Paras Passi ◽  
Mohit Singla ◽  
Nitin Gupta ◽  
...  
Keyword(s):  
Pulmonary Hypertension ◽  
Receptor Antagonist ◽  
Progressive Disease ◽  
Pulmonary Artery Hypertension ◽  
Functional Class ◽  
Endothelin Receptor Antagonist ◽  
Endothelin Receptor ◽  
Endothelin System ◽  
Exercise Endurance ◽  
Orally Active

Activation of the endothelin system has been demonstrated in the plasma and lung tissue of PAH (Pulmonary Artery Hypertension) patients. Although it is not clear if the increases in endothelin plasma levels are a cause or a consequence of PH (Pulmonary Hypertension), the data supports a prominent role for the endothelin system in the pathogenesis of PAH. Bosentan is an endothelin receptor antagonist used in the treatment of Primary pulmonary hypertension (PPH) which is a progressive disease with high mortality and administration of the orally active, dual endothelin receptor antagonist bosentan improves exercise endurance, haemodynamics, and functional class over the short term. First-line bosentan therapy was found to improve survival in patients with advanced primary pulmonary hypertension.International Journal of Human and Health Sciences Vol. 03 No. 01 January’19. Page : 10-13

Pathophysiological role of endothelin revealed by the first orally active endothelin receptor antagonist

Nature ◽  
1993 ◽  
Vol 365 (6448) ◽  
pp. 759-761 ◽  
Author(s):  
Martine Clozel ◽  
Volker Breu ◽  
Kaspar Burri ◽  
Jean-Marie Cassal ◽  
Walter Fischli ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Endothelin Receptor Antagonist ◽  
Endothelin Receptor ◽  
Pathophysiological Role ◽  
Orally Active
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