Endothelin antagonism with bosentan: Current status and future perspectives

Cardiovascular Drug Reviews

Volumn 20, Issue 1, 2002, Pages 1-18

  Ono, Koh ^a   Matsumori, Akira ^a  

^a KYOTO UNIVERSITY   (Japan)

Author keywords

Congestive heart failure; Endothelin receptor antagonist; Hypertension

Indexed keywords

2 BUTYL 7 [2 (2 CARBOXYPROPYL) 4 METHOXYPHENYL] 5 (3,4 METHYLENEDIOXYPHENYL)CYCLOPENTENO[1,2 B]PYRIDINE 6 CARBOXYLIC ACID; BMS 193884; BOSENTAN; CYCLO(DEXTRO TRYPTOPHYL DEXTRO ASPARTYLPROLYL DEXTRO VALYLLEUCYL); DARUSENTAN; DIPEPTIDYL CARBOXYPEPTIDASE INHIBITOR; ENDOTHELIN; ENDOTHELIN RECEPTOR; ENDOTHELIN RECEPTOR ANTAGONIST; L 754142; UNCLASSIFIED DRUG; WARFARIN;

BRAIN VASOSPASM; CONGESTIVE HEART FAILURE; DRUG EFFICACY; DRUG METABOLISM; DRUG SAFETY; DRUG STRUCTURE; EDEMA; FLUSHING; HEADACHE; HUMAN; HYPERTENSION; HYPOTENSION; LIVER TOXICITY; PATHOGENESIS; PRIORITY JOURNAL; REVIEW; TREATMENT PLANNING;

EID: 0036073071     PISSN: 08975957     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.1527-3466.2002.tb00078.x     Document Type: Review

References (150)

1. Metabolism of endothelin-1 and big endothelin-1 by recombinant neutral endopeptidase EC.3.4.24.11
2. Role of neutral endopeptidase in the metabolism of endothelin
3. Cloning and expression of a CDNA encoding an endothelin receptor
4. Endothelin and the production of cerebral vasospasm in dogs
5. Effect of an endothelin antagonist on hemodynamic responses to angiotensin 11
6. Therapeutic effects of endothelin receptor antagonists in stroke
7. Bosentan ameliorates cyclosporin A-induced hypertension in rats and primates
8. ET(A) receptor blockade prevents increased tissue endothelin-1, vascular hypertrophy, and endothelial dysfunction in salt-sensitive hypertension
9. Endothelin ETA receptor blockade restores NO-mediated endothelial function and inhibits atherosclerosis in apolipoprotein E-deficient mice
10. Angiotensin 11 increases vascular and renal endothelin-1 and functional endothelin converting enzyme activity in vivo: Role of ETA receptors for endothelin regulation
11. Renoprotective effect of contemporary blocking of angiotensin II and endothelin-1 in rats with membranous nephropathy
12. Blocking both type A and B endothelin receptors in the kidney attenuates renal injury and prolongs survival in rats with remnant kidney
13. Release of endothelin from the porcine aorta. Inhibition by endothelium-derived nitric oxide
14. Oxidized low density lipoproteins induce mRNA expression and release of endothelin from human and porcine endothelium
15. Role of endothelin in mediating neurogenic plasma extravasation in rat dura mater
16. Bosentan prevents preglomerular alterations during angiotensin II hypertension
17. Endothelin in experimental congestive heart failure in the anesthetized dog
18. Endothelin-receptor antagonist bosentan prevents and reverses hypoxic pulmonary hypertension in rats
19. Cranial and cardiac neural crest defects in endothelin-A receptor-deficient mice
20. Pharmacological characterization of bosentan, a new potent orally active nonpeptide endothelin receptor antagonist
21. The endothelin ETB receptor mediates both vasodilation and vasoconstriction in vivo
22. Effects of nonpeptide endothelin receptor antagonists in rats with reduced renal mass
23. 3H]bosentan binding to human coronary artery: Functional correlates
24. Endothelin stimulated by angiotensin II augments contractility of spontaneously hypertensive rat resistance arteries
25. Role of endogenous endothelin-1 in experimental renal hypertension in dogs
26. Endothelin antagonists in salt-dependent hypertension associated with renal insufficiency
27. Human pulmonary circulation is an important site for both clearance and production of endothelin-1
28. Protection from pulmonary hypertension with an orally active endothelin receptor antagonist in hypoxic rats
29. Selective upregulation of endothelin converting enzyme-1a in the human failing heart
30. Racial differences in plasma endothelin-1 concentrations in individuals with essential hypertension
31. Chronic renal failure following liver transplantation: A retrospective analysis
32. Cyclosporin A increases basal intracellular calcium and calcium responses to endothelin and vasopressin in human coronary myocytes
33. Clearance of circulating endothelin-1 by ETB receptors in rats
34. Endothelin-1 enhances calcium entry through T-type calcium channels in cultured neonatal rat ventricular myocytes
35. Effects of bosentan (Ro 47-0203), an ETA-, ETB-receptor antagonist, on regional haemodynamic responses to endothelins in conscious rats
36. Effects of Ro 47-0203 on endothelin-1 and sarafotoxin S6cinduced contractions of human bronchus and guinea-pig trachea
37. Expression of endothelin-1 in the lungs of patients with pulmonary hypertension
38. An orally active ETA/ETB receptor antagonist ameliorates proteinuria and glomerular lesions in rats with proliferative nephritis
39. Bosentan improves renal regional blood flow in rats with experimental congestive heart failure
40. Bosentan in essential hypertension
41. Effects of Ro 47-0203 and PD155080 on the plasma kinetics, receptor binding and vascular effects of endothelin in the pig
42. Telemetry monitoring of pulmonary arterial pressure in freely moving rats
43. Hypoxia increases endothelin release in bovine endothelial cells in culture, but epinephrine, norepinephrine, serotonin, histamine and angiotensin II do not
44. Prospective, randomized, double-blind trial of BQ-123 and bosentan for prevention of vasospasm following subarachnoid hemorrhage in monkeys
45. Endothelin is a potent mitogen for rat vascular smooth muscle cells
46. Effects of endothelin receptor antagonists on the progression of diabetic nephropathy
47. Endothelin-1 transgenic mice develop glomerulosclerosis, interstitial fibrosis, and renal cysts but not hypertension
48. A homozygous mutation in the endothelin-3 gene associated with a combined Waardenburg type 2 and Hirschsprung phenotype (Shah-Waardenburg syndrome)
49. The endothelin antagonist bosentan: Hemodynamic effects during normoxia and hypoxic pulmonary hypertension in pigs
50. Targeted and natural (piebald-lethal) mutations of endothelin-B receptor gene produce megacolon associated with spotted coat color in mice
51. Coexpression of endothelin-converting enzyme-1 and endothelin-1 in different stages of human atherosclerosis
52. Phosphoramidon, a metalloproteinase inhibitor, suppresses the secretion of endothelin-1 from cultured endothelial cells by inhibiting a big endothelin-1 converting enzyme
53. The human endothelin family: Three structurally and pharmacologically distinct isopeptides predicted by three separate genes
54. The human preproendothelin-1 gene. Complete nucleotide sequence and regulation of expression
55. Endothelin-1 is an autocrine/paracrine factor in the mechanism of angiotensin II-induced hypertrophy in cultured rat cardiomyocytes
56. Endothelin B receptor deficiency potentiates ET-1 and hypoxic pulmonary vasoconstriction
57. Differential effects of angiotensin II of versus endothelin-1 inhibitions in hypertrophic left ventricular myocardium during transition to heart failure
58. Endothelin stimulates multiple responses in isolated adult ventricular cardiac myocytes
59. Role of blood pressure in the development of congestive heart failure. The Framingham study
60. Cytokine stimulated endothelin release from endothelial cells
61. Role of endothelin in acute renal failure due to rhabdomyolysis in rats
62. Respective role of humoral factors and blood pressure in cardiac remodeling of DOCA hypertensive rats
63. Sarafotoxin receptors mediate phosphoinositide hydrolysis in various rat brain regions
64. In vitro effect of endothelin-1 on collagen, and ADP-induced aggregation in human whole blood and platelet rich plasma
65. Regional hemodynamic and baroreflex effects of endothelin in rats
66. Hypoxia induces endothelin gene expression and secretion in cultured human endothelium
67. Renal endothelin system in obstructive jaundice: Its role in impaired renal function of bile-duct ligated rats
68. The effect of an endothelin-receptor antagonist, bosentan, on blood pressure in patients with essential hypertension
69. Aortic arch malformations and ventricular septal defect in mice deficient in endothelin-1
70. Elevated blood pressure and craniofacial abnormalities in mice deficient in endothelin-1
71. Long-term open-label experience with an endothelin receptor antagonist, bosentan, in patients with severe chronic heart failure
72. Endothelin gene variants and aortic and cardiac structure in never-treated hypertensives
73. Endothelin-1 expression in blood vessels of DOCA-salt hypertensive rats treated with the combined ETA/ETB endothelin receptor antagonist bosentan
74. Effect of BQ-123 and Ro 47-0203 (bosentan) on endothelin-induced vasoconstriction in the rat skin
75. Circulating and tissue endothelin immunoreactivity in advanced atherosclerosis
76. Comparison of effect of endothelin antagonism and angiotensin-converting enzyme inhibition on blood pressure and vascular structure in spontaneously hypertensive rats treated with N omega-nitro-L-arginine methyl ester. Correlation with topography of vascular endothelin-1 gene expression
77. Effect of a nonselective endothelin antagonist on vascular remodeling in deoxycorticosterone acetate-salt hypertensive rats. Evidence for a role of endothelin in vascular hypertrophy
78. Chronic endothelin receptor antagonist treatment of young spontaneously hypertensive rats
79. Effect of chronic treatment of adult spontaneously hypertensive rats with an endothelin receptor antagonist
80. Renal and vascular effects of chronic endothelin receptor antagonism in malignant hypertensive rats
81. Cloning and functional expression of a vascular smooth muscle endothelin 1 receptor
82. Effect of endothelin-1 on neutrophil adhesion to endothelial cells and perfused heart
83. Interaction between endothelin-1 and endothelium-derived relaxing factor in human arteries and veins
84. Contrasting inotropic effects of endogenous endothelin in the normal and failing human heart: Studies with an intracoronary ET(A) receptor antagonist
85. Increased endothelin in experimental heart failure
86. Plasma endothelin in chronic heart failure
87. Paracrine effects of endocardial endothelial cells on myocyte contraction mediated via endothelin
88. Integrated cardiac, renal, and endocrine actions of endothelin
89. Endothelin-converting enzyme expression in the rat vascular injury model and human coronary atherosclerosis
90. Age- and sex-related variation of plasma endothelin-1 concentration in normal and hypertensive subjects
91. Increased plasma concentrations of endothelin-1 and big endothelin-1 in acute myocardial infarction
92. Angiotensin II increases tissue endothelin and induces vascular hypertrophy: Reversal by ET(A)-receptor antagonist
93. Role of endogenous endothelin in chronic heart failure: Effect of long-term treatment with an endothelin antagonist on survival, hemodynamics, and cardiac remodeling
94. Effect of a specific endothelin A receptor antagonist on murine lupus nephritis
95. Endothelin-1 production and decreased endothelin B receptor expression in advanced prostate cancer
96. Identification of endothelin-1 in the pathophysiology of metastatic adenocarcinoma of the prostate
97. Polymorphisms of the endothelin-A and -B receptor genes in relation to blood pressure and myocardial infarction: The Etude Cas-Temoins sur l'Infarctus du Myocarde (ECTIM) Study
98. Increased activation of sympathetic nervous system and endothelin by mental stress in normotensive offspring of hypertensive parents
99. Purification and characterization of a phosphoramidonsensitive endothelin-converting enzyme in porcine aortic endothelium
100. Cytokine-induced release of endothelin-1 from porcine renal epithelial cell line
101. Bosentan, an orally active endothelin antagonist: Effect on the renal response to contrast media
102. Plasma endothelin determination as a prognostic indicator of 1-year mortality after acute myocardial infarction
103. Contribution of endothelin-1 to myocardial injury in a murine model of myocarditis: Acute effects of bosentan, an endothelin receptor antagonist
104. ETB-mediated regulation of extracellular levels of endothelin-1 in cultured human endothelial cells
105. Multicenter, double-blind, placebo-controlled study of long-term endothelin blockade with bosentan in chronic heart failure-Results of the REACH-1 trial
106. Abnormal endothelium-dependent vascular relaxation in patients with essential hypertension
107. A missense mutation of the endothelin-B receptor gene in multigenic Hirschsprung's disease
108. 2+ and contractility in single ventricular myocytes from the ferret and human
109. The role of endothelin in experimental cerebral vasospasm
110. Tissue endothelin-converting enzyme activity correlates with cardiovascular risk factors in coronary artery disease
111. Increased plasma endothelin level in patients with essential hypertension
112. Endogenous endothelin-1 participates in the maintenance of cardiac function in rats with congestive heart failure. Marked increase in endothelin-1 production in the failing heart
113. Cloning of a cDNA encoding a non-isopeptide-selective subtype of the endothelin receptor
114. Deoxycorticosterone acetate plus salt induces overexpression of vascular endothelin-1 and severe vascular hypertrophy in spontaneously hypertensive rats
115. Antihypertensive effect of an endothelin receptor antagonist in DOCA-salt spontaneously hypertensive rats
116. Both ETA and ETB receptors mediate contraction to endothelin-1 in human blood vessels
117. Quantitative association between a newly identified molecular variant in the endothelin-2 gene and human essential hypertension
118. The effect of bosentan, a new potent endothelin receptor antagonist, on the pathogenesis of cerebral vasospasm
119. Cloning and functional expression of endothelin-converting enzyme from rat endothelial cells
120. Short-term hemodynamic effects of endothelin receptor blockade in dogs with chronic heart failure
121. Acute pulmonary alveolar hypoxia increases lung and plasma endothelin-1 levels in conscious rats
122. Differential regulation of fos and jun gene expression and AP-1 ciselement activity by endothelin isopeptides. Possible implications for mitogenic signaling by endothelin
123. Systemic and renal effect of intravenous infusion of endothelin-1 in healthy human volunteers
124. Genetic variability of the ET-1 and the ETA receptor genes in essential hypertension
125. Increased plasma endothelin-1 in pulmonary hypertension: Marker or mediator of disease?
126. Endothelin ETA and ETB receptors mediate vascular smooth muscle contraction
127. Short-term oral endothelin-receptor antagonist therapy in conventionally treated patients with symptomatic severe chronic heart failure
128. The role of endothelin-1 in the origin of cerebral vasospasm in patients with aneurysmal subarachnoid hemorrhage
129. Vasoconstriction to endogenous endothelin-1 is increased in the peripheral circulation of patients with essential hypertension
130. Purification and characterization of endothelin-converting enzyme from rat lung
131. Endothelin receptor is coupled to phospholipase C via a pertussis toxin-insensitive guanine nucleotide-binding regulatory protein in vascular smooth muscle cells
132. Role of endogenous endothelin in normal hemodynamic status of anesthetized dogs
133. An overview of contemporary etiologies of congestive heart failure
134. The Lys 198 Asn polymorphism in the endothelin-1 gene is associated with blood pressure in overweight people
135. Characterization of contractile endothelin and angiotensin receptors in human resistance arteries: Evidence for two endothelin and one angiotensin receptor
136. Bosentan, a new endothelin receptor antagonist: Prediction of the systemic plasma clearance in man from combined in vivo and in vitro data
137. Central effects of endothelin on baroreflex of spontaneously hypertensive rats
138. Say NO to ET
139. Effects of the endothelin antagonist bosentan in patients with elevated Doppler velocities after aneurysmal SAH
140. Protective effects of non-peptide endothelin receptor antagonist bosentan on myocardial ischaemic and reperfusion injury in the pig
141. Absorption, excretion, and metabolism of the endothelin receptor antagonist bosentan in healthy male subjects
142. Endothelin in human congestive heart failure
143. Bosentan-improved cardiopulmonary vascular performance and increased plasma levels of endothelin-1 in porcine endotoxin shock
144. A novel potent vasoconstrictor peptide produced by vascular endothelial cells
145. Hemodynamic shear stress stimulates endothelin production by cultured endothelial cells
146. Endothelin in cerebral vasospasm. Clinical and experimental results
147. Prevention of cerebral vasospasm after experimental subarachnoid hemorrhage by Ro 47-0203, a newly developed orally active endothelin receptor antagonist
148. Increased plasma endothelin-1 in acute ischemic stroke
149. Passive Heymann nephritis: Evidence that angiotensin-converting enzyme inhibition reduces proteinuria and retards renal structural injury
150. Prevention of subarachnoid hemorrhage-induced cerebral vasospasm by oral administration of endothelin receptor antagonists