Results 281 to 290 of about 40,821 (327)

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
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[Endothelin receptor antagonist].

Nihon rinsho. Japanese journal of clinical medicine, 2009
Pulmonary arterial hypertension(PAH) is an uncommon disease characterised by a progressive increase in pulmonary vascular resistance. An imbalance between vasoconstrictor/vasodilator activities could be responsible for altered pulmonary vascular tone and structure. In PAH patients, endothelin are increased.
Takuya, Kishi, Kenji, Sunagawa
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Heart failure and endothelin receptor antagonists

Trends in Pharmacological Sciences, 1999
Cardiac myocytes and vascular endothelial cells produce endothelin-1, which increases the contractility of cardiac muscles and of vascular smooth muscles. Endothelin-1 also exerts long-term effects, such as myocardial hypertrophy, and causes cellular injury in cardiac myocytes.
T, Miyauchi, K, Goto
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Endothelin-Receptor Antagonists in Uremic Cardiomyopathy

Journal of Cardiovascular Pharmacology, 2000
Increased endothelin-1 (ET-1) levels were found in patients with chronic renal failure. These correlate with the severity of renal failure. Patients with elevated ET-1 concentrations show an increased cardiovascular mortality. The prevalence of severe left ventricular hypertrophy (LVH) is a very important factor for survival and morbidity in uremic ...
S C, Wolf, F, Gaschler, S, Brehm, M, Klaussner, K, Amann, T, Risler, B R, Brehm   +6 more
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Endothelin Receptors and Receptor Antagonists

1998
Multiple receptor subtypes for endothelin have been identified in pharmacological studies both in vitro and in vivo. As can be evidenced in the study by Yanagisawa et al, at least two receptor subtypes may be responsible for the biphasic nature of the hemodynamic response to intravenous injection of ET-1: a transient hypotension followed by a sustained
Andrew S. Tasker, David M. Pollock
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Endothelin and Endothelin Receptor Antagonists in Heart Failure

Congestive Heart Failure, 2002
Endothelin (ET) is a recently discovered 21‐amino acid peptide that has potent physiologic and pathophysiologic effects that appear to be involved in the development of heart failure. These include effects on arterial smooth muscle cells that cause intense peripheral vasoconstriction and stimulation of cardiac myocytes and fibroblasts.
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Endothelin Receptor Antagonists in Cancer Therapy

Cancer Investigation, 2007
Endothelins are a family of peptide compounds which exert regulatory control over cellular processes important for growth, survival, invasion, and angiogenesis. In particular, endothelin-1, acting primarily through the endothelin-A receptor, is implicated in the neoplastic growth of multiple tumor types.
Mihailo, Lalich, Douglas G, McNeel, George, Wilding, Glenn, Liu   +3 more
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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 ...
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Endothelins and endothelin receptor antagonists: Binding to plasma proteins

Life Sciences, 1996
Endothelins (ET) are 21-amino acid peptides that bind to membrane receptors to initiate a wide range of pathophysiological effects. PD-156707, L-749329, Ro-470203, and A-127722 are potent non-peptide ET receptor antagonists developed recently. When tested in human and rat plasma, both ET-1 and -3 and the four aforementioned antagonists exhibited a high
J R, Wu-Wong, W J, Chiou, D J, Hoffman, M, Winn, T W, von Geldern, T J, Opgenorth   +5 more
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Endothelin Receptor Antagonist

2017
Endothelin (ET)-1, a peptide mainly produced by vascular endothelial cells, has potent and long-lasting vasoconstrictive effect. In addition, ET-1 has been shown to induce a variety of biological effects including cell proliferation, inflammation, and fibrosis.
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