Results 211 to 220 of about 18,729 (264)

Bis-sulfonamides as endothelin receptor antagonists

Bioorganic & Medicinal Chemistry Letters, 2003
Modification of the structure of bosentan 1, the first marketed endothelin receptor antagonist (Tracleer), by introduction of a second sulfonamide function at the alkoxy side chain, led to bis-sulfonamides 2. This allowed to prepare dual ET(A)/ET(B) as well as ET(B) receptor selective antagonists, which could serve as tools to investigate the ...
Christoph, Boss, Martin H, Bolli, Thomas, Weller, Walter, Fischli, Martine, Clozel   +4 more
openaire   +2 more sources

Endothelin, endothelin receptors, and endothelin antagonists.

Current opinion in nephrology and hypertension, 1995
Endothelin 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 ...
openaire   +1 more source

Bosentan: a dual endothelin receptor antagonist

Expert Opinion on Investigational Drugs, 2002
The peptide endothelin plays a significant role in a wide array of pathological conditions, including primary pulmonary hypertension and pulmonary arterial hypertension associated with collagen vascular disease. These are life-threatening conditions that can severely compromise the function of the lungs and heart.
Lewis J, Rubin, Sébastien, Roux
openaire   +2 more sources

Pharmacology of tezosentan, new endothelin receptor antagonist designed for parenteral use.

Journal of Pharmacology and Experimental Therapeutics, 1999
Tezosentan (Ro 61-0612) [5-isopropyl-pyridine-2-sulfonic acid 6-(2-hydroxy-ethoxy)-5-(2-methoxy-phenoxy)-2-(2-1H-tetrazol-5-yl-+ ++pyri din-4-yl)-pyrimidin-4-ylamide] is a new endothelin (ET) receptor antagonist specifically designed for parenteral use ...
M. Clozel, H. Ramuz, J. Clozel, Volker Breu, Patrick Hess, B. Löffler, P. Coassolo, Sébastien Roux   +7 more
semanticscholar   +1 more source

Update on Endothelin Receptor Antagonists in Hypertension

Current Hypertension Reports, 2018
To review the most recent data on the development of endothelin receptor antagonists (ERAs) for the treatment of hypertension and the management of diabetic nephropathy RECENT FINDINGS: Recent reviews and meta-analyses of experimental and clinical data obtained with ERAs confirmed that endothelin receptor blockade is associated with significant ...
openaire   +3 more sources

Endothelin receptor antagonists: a brief review

Canadian Journal of Physiology and Pharmacology, 1994
The endothelins are a family of potent vasoconstrictors, some of which also have vasodilatory activity. In many diseases associated with tissue hypoxia or ischemia and in diseases in which vasoconstriction plays a role, the circulating levels of endothelin are higher than in healthy, control subjects.
openaire   +2 more sources

Bosentan, a mixed endothelin receptor antagonist, inhibits superoxide anion-induced pain and inflammation in mice

Naunyn-Schmiedeberg's Archives of Pharmacology, 2015
K. G. Serafim, Suelen A. Navarro, Ana C Zarpelon, Felipe A. Pinho-Ribeiro, V. Fattori, T. Cunha, J. Alves-Filho, F. Cunha, R. Casagrande, W. Verri   +9 more
semanticscholar   +1 more source

X-ray structures of endothelin ETB receptor bound to clinical antagonist bosentan and its analog

Nature Structural &Molecular Biology, 2017
W. Shihoya, T. Nishizawa, K. Yamashita, A. Inoue, K. Hirata, Francois Marie Ngako Kadji, Akiko Okuta, K. Tani, J. Aoki, Y. Fujiyoshi, T. Doi, O. Nureki   +11 more
semanticscholar   +1 more source

Oral treprostinil for the treatment of pulmonary arterial hypertension in patients receiving background endothelin receptor antagonist and phosphodiesterase type 5 inhibitor therapy (the FREEDOM-C2 study): a randomized controlled trial.

Chest, 2013
V. Tapson, Z. Jing, Kaifeng Xu, L. Pan, J. Feldman, D. Kiely, E. Kotlyar, C. McSwain, K. Laliberte, C. Arneson, Lewis J. Rubin   +10 more
semanticscholar   +1 more source

Safety, tolerability, pharmacokinetics, and pharmacodynamics of macitentan, an endothelin receptor antagonist, in an ascending multiple‐dose study in healthy subjects

Journal of clinical pharmacology, 2013
P. Sidharta, P. V. van Giersbergen, J. Dingemanse   +2 more
semanticscholar   +1 more source