Results 191 to 200 of about 18,729 (264)

Peptoids as endothelin receptor antagonists

Bioorganic & Medicinal Chemistry Letters, 2001
A series of new peptoids as endothelin receptor antagonists has been synthesized. Screening them for their ability to bind with endothelin receptors (ET(A) and ET(B)) competitively in the presence of (125I) endothelin led to the discovery of compounds as possible leads with IC50s in the low micromolar concentrations.
F, Dasgupta, N, Gangadhar, M, Bruhaspathy, A K, Verma, S, Sarin, A K, Mukherjee   +5 more
openaire   +2 more sources

Endothelin Receptor Antagonists - An Overview

Current Medicinal Chemistry, 2002
In thirteen years since the appearance of Endothelin (ET) on the international scene, possibility of its involvement in a variety of diseases has attracted the attention of medicinal chemists in search of novel therapeutics for various cardiovascular diseases (CVDs).
Falguni, Dasgupta, Ashis K, Mukherjee, N, Gangadhar   +2 more
openaire   +2 more sources

Ambrisentan, an endothelin receptor type A-selective endothelin receptor antagonist, for the treatment of pulmonary arterial hypertension

Expert Opinion on Pharmacotherapy, 2009
Martha Kingman
exaly   +2 more sources

Endothelin Receptor Antagonists

2013
Three pathways have been identified in the pathogenesis of pulmonary arterial hypertension (PAH): the endothelin (ET), nitric oxide (NO) and prostacyclin pathways. These pathways represent the targets of approved PAH therapies and their discovery has facilitated significant progress in the understanding and treatment of PAH.
Martine, Clozel, Alessandro, Maresta, Marc, Humbert   +2 more
openaire   +2 more sources

Endothelin receptor antagonist for subarachnoid haemorrhage

Cochrane Database of Systematic Reviews, 2010
A subarachnoid hemorrhage (SAH) is a serious and potentially life-threatening condition where blood leaks out of blood vessels over the surface of the brain. Delayed ischemic neurological deficit (DIND) and the related feature of vasospasm, where patients experience a delayed deterioration, have long been recognized as the leading potentially treatable
Jia, Guo, Zhenghong, Shi, Kehu, Yang, Jin Hui, Tian, Lei, Jiang   +4 more
openaire   +2 more sources

Nonpeptide endothelin receptor antagonists. XI. Pharmacological characterization of SB 234551, a high-affinity and selective nonpeptide ETA receptor antagonist.

Journal of Pharmacology and Experimental Therapeutics, 1998
The present study describes the pharmacological profile of ((E)-alpha-[[1-butyl-5-[2-[(2-carboxyphenyl)methoxy]-4-methoxy-phenyl ]-1H-pyrazol-4-yl]methlene]-6-methoxy-1,3-benzodioxole-5-propanoic acid) (SB 234551), a high-affinity, nonpeptide endothelin ...
E. Ohlstein, Ponnal Nambi, Douglas W. P. Hay, Miklos Gellai, David P. Brooks, Juan I. Luengo, Jia Xiang, John D. Elliott   +7 more
semanticscholar   +1 more source

Endothelin, endothelin receptors, and endothelin antagonists

Current Opinion in Nephrology and Hypertension, 1994
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

Pharmacological characterization of bosentan, a new potent orally active nonpeptide endothelin receptor antagonist.

Journal of Pharmacology and Experimental Therapeutics, 1994
The authors describe here the pharmacological properties of bosentan, a new nonpeptide mixed antagonist of endothelin (ET) receptors, obtained by structural optimization of the less potent Ro 46-2005 [Ro 46-2005 (4-tert-butyl-N-[6-(2-hydroxyethoxy)-5-(3 ...
M. Clozel, V. Breu, G. Gray, B. Kalina, B. Löffler, K. Burri, J. Cassal, G. Hirth, Marcel Muller, Werner L. Neidhart   +9 more
semanticscholar   +1 more source

Enrasentan, an Antagonist of Endothelin Receptors

Cardiovascular Drug Reviews, 2003
ABSTRACTEndothelins are powerful vasoconstrictor agents produced by endothelial cells and identified by Yanagisawa et al. in 1988. Two types of receptors for endothelins have been identified: ETAreceptors are located on smooth muscle cells of the vascular wall and are responsible for endothelin‐induced vasoconstriction while ETBreceptors are located on
openaire   +3 more sources

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.
openaire   +2 more sources