Endothelin Receptor Antagonists and Cerebral Vasospasm: An Update

THIS REVIEW UPDATES the current status of endothelin receptor antagonists in the treatment of cerebral vasospasm. Recent preclinical and clinical studies are reviewed, as well as clinical trials for other medical indications. Some of the newer endothelin receptor antagonists are also examined.

[1]  D. Stewart,et al.  Human pulmonary circulation is an important site for both clearance and production of endothelin-1. , 1996, Circulation.

[2]  L. Noble,et al.  Involvement of the endothelin receptor subtype A in neuronal pathogenesis after traumatic brain injury , 1998, Brain Research.

[3]  G. Sutherland,et al.  Augmentation of endothelial function by endothelin antagonism in human saphenous vein conduits. , 2001, Journal of neurosurgery.

[4]  R. Macdonald,et al.  Increased Expression of Endothelin B Receptor mRNA following Subarachnoid Hemorrhage in Monkeys , 1996, Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism.

[5]  R. Largo,et al.  An orally active ETA/ETB receptor antagonist ameliorates proteinuria and glomerular lesions in rats with proliferative nephritis. , 1996, Kidney international.

[6]  M. Zimmermann Endothelin in cerebral vasospasm. Clinical and experimental results. , 1997, Journal of neurosurgical sciences.

[7]  S. Nakanishi,et al.  Molecular cloning of a non-isopeptide-selective human endothelin receptor. , 1991, Biochemical and biophysical research communications.

[8]  M. Zuccarello,et al.  Endothelin B receptor antagonists attenuate subarachnoid hemorrhage-induced cerebral vasospasm. , 1998, Stroke.

[9]  W. Neidhart,et al.  Ro 61-1790, a new hydrosoluble endothelin antagonist: general pharmacology and effects on experimental cerebral vasospasm. , 1997, The Journal of pharmacology and experimental therapeutics.

[10]  J. Michel,et al.  A fourth isoform of endothelin-converting enzyme (ECE-1) is generated from an additional promoter molecular cloning and characterization. , 1999, European journal of biochemistry.

[11]  T. Hamakubo,et al.  Modulatory effects of endothelin on baroreflex activation in the nucleus of the solitary tract. , 1998, European journal of pharmacology.

[12]  P. Macdonald,et al.  Hemodynamic effects of Bosentan, an endothelin receptor antagonist, in patients with pulmonary hypertension. , 2000, Circulation.

[13]  J. Vane,et al.  Endothelin-1 release from endothelial cells in culture is elevated both acutely and chronically by short periods of mechanical stretch. , 1994, Biochemical and biophysical research communications.

[14]  C. Gomez-Sanchez,et al.  Hypoxia increases endothelin release in bovine endothelial cells in culture, but epinephrine, norepinephrine, serotonin, histamine and angiotensin II do not. , 1990, Life sciences.

[15]  R. Simari,et al.  Autocrine role for the endothelin-B receptor in the secretion of adrenomedullin. , 1998, Hypertension.

[16]  C. Goresky,et al.  Pulmonary clearance of circulating endothelin-1 in dogs in vivo: exclusive role of ETB receptors. , 1996, Journal of applied physiology.

[17]  M. Zuccarello,et al.  Endothelin ETA and ETB receptors in subarachnoid hemorrhage-induced cerebral vasospasm. , 1994, European journal of pharmacology.

[18]  J. Vane,et al.  Pressor effects of circulating endothelin are limited by its removal in the pulmonary circulation and by the release of prostacyclin and endothelium-derived relaxing factor. , 1988, Proceedings of the National Academy of Sciences of the United States of America.

[19]  Y. Yazaki,et al.  Hemodynamic shear stress stimulates endothelin production by cultured endothelial cells. , 1989, Biochemical and biophysical research communications.

[20]  J. Yoshikawa,et al.  Effect of the endothelin family of peptides on human coronary artery smooth-muscle cell migration. , 1998, Journal of cardiovascular pharmacology.

[21]  I. Miyamori,et al.  Interleukin-2 enhances the release of endothelin-1 from the rat mesenteric artery. , 1991, Life sciences.

[22]  Sadao Kimura,et al.  A novel potent vasoconstrictor peptide produced by vascular endothelial cells , 1988, Nature.

[23]  M. Zuccarello,et al.  Decreased endothelium-dependent relaxation in subarachnoid hemorrhage-induced vasospasm: role of ET-1. , 1995, The American journal of physiology.

[24]  S. Gottlieb,et al.  Acute endothelin A receptor blockade causes selective pulmonary vasodilation in patients with chronic heart failure. , 2000, Circulation.

[25]  L. V. von Segesser,et al.  Interaction between endothelin-1 and endothelium-derived relaxing factor in human arteries and veins. , 1990, Circulation research.

[26]  R. Macdonald,et al.  Prevention of vasospasm after subarachnoid hemorrhage in dogs by continuous intravenous infusion of PD156707. , 1998, Neurologia medico-chirurgica.

[27]  K. Kikkawa,et al.  Prevention of cerebral vasospasm by a novel endothelin receptor antagonist, TA-0201. , 1999, Journal of cardiovascular pharmacology.

[28]  R. Paul,et al.  Eicosonoid metabolism and beta-adrenergic mechanisms in coronary arterial smooth muscle: potential compartmentation of cAMP. , 1986, The American journal of physiology.

[29]  J. Vane,et al.  Endothelin‐1 and Endothelin‐3 Release EDRF from Isolated Perfused Arterial Vessels of the Rat and Rabbit , 1989, Journal of Cardiovascular Pharmacology.

[30]  D. Faller,et al.  Hypoxia induces endothelin gene expression and secretion in cultured human endothelium. , 1991, The Journal of clinical investigation.

[31]  R. Willette,et al.  Nonpeptide Endothelin Antagonist: Cerebrovascular Characterization and Effects on Delayed Cerebral Vasospasm , 1994, Stroke.

[32]  R. Macdonald,et al.  Effect of BQ-123 and tissue plasminogen activator on vasospasm after subarachnoid hemorrhage in monkeys. , 1996, Stroke.

[33]  L. Reisin,et al.  The dual endothelin receptor antagonist tezosentan acutely improves hemodynamic parameters in patients with advanced heart failure. , 2001, American heart journal.

[34]  M. Fujimoto,et al.  Effects of an endothelin ET(A)-receptor antagonist, S-0139, on cerebral vasospasm and behavioral changes in dogs intracisternally administered endothelin-1. , 1998, Life sciences.

[35]  Hawkey,et al.  Protection against aspirin‐induced human gastric mucosal injury by bosentan, a new endothelin‐1 receptor antagonist , 1999, Alimentary pharmacology & therapeutics.

[36]  D. Webb,et al.  Nitric Oxide Synthesis and by Endothelin-B Receptor Blockade Mediated Vasodilatation Is Attenuated by Inhibition of − Endothelin-A Receptor Antagonist , 1998 .

[37]  B. Binder,et al.  Polar secretion of endothelin-1 by cultured endothelial cells. , 1992, The Journal of biological chemistry.

[38]  Y. Ueta,et al.  Effects of centrally administered endothelin-3 on renal sympathetic nerve activity and renal blood flow in conscious rats. , 1994, Journal of the autonomic nervous system.

[39]  P. Hunziker,et al.  Short-term oral endothelin-receptor antagonist therapy in conventionally treated patients with symptomatic severe chronic heart failure. , 1998, Circulation.

[40]  R. Ikegawa,et al.  Phosphoramidon prevents cerebral vasospasm following subarachnoid hemorrhage in dogs: the relationship to endothelin-1 levels in the cerebrospinal fluid. , 1991, Life sciences.

[41]  S. S. Sørensen,et al.  Systemic and renal effect of intravenous infusion of endothelin-1 in healthy human volunteers. , 1994, The American journal of physiology.

[42]  K. Tanzawa,et al.  Identification and characterization of two isoforms of an endothelin‐converting enzyme‐1 , 1995, FEBS letters.

[43]  M. Clozel Endothelin receptor antagonists: current status and perspectives. , 2000, Journal of cardiovascular pharmacology.

[44]  W. Neidhart,et al.  Pathophysiological role of endothelin revealed by the first orally active endothelin receptor antagonist , 1993, Nature.

[45]  M. Buuse,et al.  Central effects of endothelin on baroreflex of spontaneously hypertensive rats , 1993, Journal of hypertension.

[46]  T. Lüscher,et al.  Oxidized low density lipoproteins induce mRNA expression and release of endothelin from human and porcine endothelium. , 1992, Circulation research.

[47]  F. Abboud,et al.  Suppression of baroreceptor discharge by endothelin at high carotid sinus pressure. , 1992, The American journal of physiology.

[48]  T. Lüscher,et al.  Angiotensin II Increases Vascular and Renal Endothelin-1 and Functional Endothelin Converting Enzyme Activityin Vivo:Role of ETAReceptors for Endothelin Regulation , 1997 .

[49]  S. Ertel,et al.  Endothelin antagonism with bosentan: a review of potential applications , 1999, Journal of Molecular Medicine.

[50]  J. Egido,et al.  Effect of endothelin-1 on neutrophil adhesion to endothelial cells and perfused heart. , 1993, Circulation.

[51]  G. Helm,et al.  Systemic administration of the endothelin-A receptor antagonist TBC 11251 attenuates cerebral vasospasm after experimental subarachnoid hemorrhage: dose study and review of endothelin-based therapies in the literature on cerebral vasospasm. , 1998, Neurosurgery.

[52]  N. Ishida,et al.  A novel peptide, vasoactive intestinal contractor, of a new (endothelin) peptide family. Molecular cloning, expression, and biological activity. , 1989, The Journal of biological chemistry.

[53]  M. Ferrari,et al.  Endothelin antagonist bosentan blocks neurogenic inflammation, but is not effective in aborting migraine attacks , 1996, Pain.

[54]  J. Pickard,et al.  An efficacy and safety study of the ETA/B receptor antagonist TAK-044 in subarachnoid hemorrhage , 2000 .

[55]  T. Yokoyama,et al.  Endothelin-1 Initiates the Development of Vasospasm after Subarachnoid Haemorrhage Through Protein Kinase C Activation, but does not Contribute to Prolonged Vasospasm , 2000, Acta Neurochirurgica.

[56]  B. Weir,et al.  Nimodipine treatment in poor-grade aneurysm patients. Results of a multicenter double-blind placebo-controlled trial. , 1988, Journal of neurosurgery.

[57]  G. Gray,et al.  Are There Different ETB Receptors Mediating Constriction and Relaxation? , 1995, Journal of cardiovascular pharmacology.

[58]  C. Goresky,et al.  Pulmonary clearance of circulating endothelin-1 in dogs in vivo: exclusive role of ETB receptors. , 1996, Journal of applied physiology.

[59]  E. Tani,et al.  Endothelin-1 of canine basilar artery in vasospasm. , 1992, Journal of neurosurgery.

[60]  V. Seifert,et al.  Endothelin and subarachnoid hemorrhage: an overview. , 1998, Neurosurgery.

[61]  T. Lüscher,et al.  Acute hemodynamic and neurohumoral effects of selective ETA receptor blockade in patients with congestive heart failure , 2000 .

[62]  T. Lüscher,et al.  Angiotensin II increases vascular and renal endothelin-1 and functional endothelin converting enzyme activity in vivo: role of ETA receptors for endothelin regulation. , 1997, Biochemical and biophysical research communications.

[63]  T. Westfall,et al.  Regional hemodynamic and baroreflex effects of endothelin in rats. , 1989, The American journal of physiology.

[64]  Weir,et al.  Prospective, randomized, double-blind trial of BQ-123 and bosentan for prevention of vasospasm following subarachnoid hemorrhage in monkeys. , 1995, Journal of neurosurgery.

[65]  F. Ruschitzka,et al.  Endothelin receptor antagonists in congestive heart failure: a new therapeutic principle for the future? , 2001, Journal of the American College of Cardiology.

[66]  S. Juvela Plasma endothelin concentrations after aneurysmal subarachnoid hemorrhage. , 2000, Journal of neurosurgery.

[67]  T. Shigeno,et al.  The effect of bosentan, a new potent endothelin receptor antagonist, on the pathogenesis of cerebral vasospasm. , 1995, Neurosurgery.

[68]  A. Asai,et al.  Prevention of delayed vasospasm by an endothelin ETA receptor antagonist, BQ-123: change of ETA receptor mRNA expression in a canine subarachnoid hemorrhage model. , 1994, Journal of neurosurgery.

[69]  V. Seifert,et al.  Prevention of cerebral vasospasm after experimental subarachnoid hemorrhage by RO 47-0203, a newly developed orally active endothelin receptor antagonist. , 1996, Neurosurgery.

[70]  S. Roux,et al.  The role of endothelin in experimental cerebral vasospasm. , 1995, Neurosurgery.

[71]  T. Lüscher,et al.  Increased activation of sympathetic nervous system and endothelin by mental stress in normotensive offspring of hypertensive parents. , 1996, Circulation.

[72]  G. Murray,et al.  Efficacy and safety of the endothelin, receptor antagonist TAK-044 in treating subarachnoid hemorrhage: a report by the Steering Committee on behalf of the UK/Netherlands/Eire TAK-044 Subarachnoid Haemorrhage Study Group. , 2000, Journal of neurosurgery.

[73]  F. Cosentino,et al.  Effect of endothelinA-receptor antagonist BQ-123 and phosphoramidon on cerebral vasospasm. , 1993, Journal of cardiovascular pharmacology.

[74]  M. Packer,et al.  MULTICENTER, DOUBLEBLIND PLACEBO CONTROLLED STUDY OF LONG TERMENDOTHELIN BLOCKADE WITH BOSENTAN IN CHRONIC HEART FAILURE RESULTS OF THE REACH-1 TRIAL. ABSTRACT , 1998 .

[75]  M. Zuccarello,et al.  Prevention of subarachnoid hemorrhage-induced cerebral vasospasm by oral administration of endothelin receptor antagonists. , 1996, Journal of neurosurgery.

[76]  M. Véniant,et al.  Acute hemodynamic effects of ciprokiren, a novel renin inhibitor, in sodium-depleted dogs. , 1995, Journal of cardiovascular pharmacology.

[77]  S. Douglas,et al.  Endothelin‐1 modulates vascular smooth muscle structure and vasomotion: Implications in cardiovascular pathology , 1993 .

[78]  K. Hosoda,et al.  Acute pulmonary alveolar hypoxia increases lung and plasma endothelin-1 levels in conscious rats. , 1991, Life sciences.

[79]  M. Clozel,et al.  BQ-123, a peptidic endothelin ETA receptor antagonist, prevents the early cerebral vasospasm following subarachnoid hemorrhage after intracisternal but not intravenous injection. , 1993, Life sciences.

[80]  H. Krum,et al.  The effect of an endothelin-receptor antagonist, bosentan, on blood pressure in patients with essential hypertension. Bosentan Hypertension Investigators. , 1998, The New England journal of medicine.

[81]  P. Vanhoutte,et al.  Flow-induced release of endothelium-derived relaxing factor. , 1986, The American journal of physiology.

[82]  T. Lüscher,et al.  Release of endothelin from the porcine aorta. Inhibition by endothelium-derived nitric oxide. , 1990, The Journal of clinical investigation.

[83]  J. Pepper,et al.  Cytokine and lipopolysaccharide stimulation of endothelin-1 release from human internal mammary artery and saphenous vein smooth-muscle cells. , 1998, Journal of cardiovascular pharmacology.

[84]  M. Shichiri,et al.  Cytokine-induced release of endothelin-1 from porcine renal epithelial cell line. , 1990, Biochemical and biophysical research communications.

[85]  W E Haefeli,et al.  Nitric oxide is responsible for flow-dependent dilatation of human peripheral conduit arteries in vivo. , 1995, Circulation.

[86]  T. Horio,et al.  Production of endothelin by cultured porcine endothelial cells: modulation by adrenaline. , 1989, Journal of hypertension. Supplement : official journal of the International Society of Hypertension.

[87]  M. Porta,et al.  Cytokine stimulated endothelin release from endothelial cells. , 1991, Life sciences.

[88]  V. Breu,et al.  Absence of ET(B)-mediated contraction in Piebald-lethal mice. , 1997, Life sciences.

[89]  M. Yanagisawa,et al.  Prevention of cerebral vasospasm by actinomycin D. , 1991, Journal of neurosurgery.

[90]  N. Kassell,et al.  Reversal of subarachnoid hemorrhage-induced vasoconstriction with an endothelin receptor antagonist. , 1994, Neurosurgery.

[91]  M. Fujimoto,et al.  Profiles of an intravenously available endothelin A-receptor antagonist, S-0139, for preventing cerebral vasospasm in a canine two-hemorrhage model. , 1998, Life sciences.

[92]  G. Remuzzi,et al.  Blocking both type A and B endothelin receptors in the kidney attenuates renal injury and prolongs survival in rats with remnant kidney. , 1996, American journal of kidney diseases : the official journal of the National Kidney Foundation.

[93]  Emma J. Mickley,et al.  Activation of endothelin ETA receptors masks the constrictor role of endothelin ETB receptors in rat isolated small mesenteric arteries , 1997, British journal of pharmacology.

[94]  R. Knöfler,et al.  In vitro effect of endothelin-1 on collagen, and ADP-induced aggregation in human whole blood and platelet rich plasma. , 1995, Thrombosis research.

[95]  E. Condom,et al.  Prevention of cold ischaemia-reperfusion injury by an endothelin receptor antagonist in experimental renal transplantation. , 1999, Nephrology, dialysis, transplantation : official publication of the European Dialysis and Transplant Association - European Renal Association.

[96]  L. V. von Segesser,et al.  Threshold concentrations of endothelin-1 potentiate contractions to norepinephrine and serotonin in human arteries. A new mechanism of vasospasm? , 1990, Circulation.

[97]  T. Lüscher,et al.  Endothelin stimulated by angiotensin II augments contractility of spontaneously hypertensive rat resistance arteries. , 1992, Hypertension.

[98]  A. Davenport,et al.  Blockade and reversal of endothelin-induced constriction in pial arteries from human brain. , 1999, Stroke.

[99]  J. Pickard,et al.  Expression of endothelin(A) receptors in human gliomas and meningiomas, with high affinity for the selective antagonist PD156707. , 1998, Neurosurgery.

[100]  T. Masaki The endothelin family: an overview. , 2000, Journal of cardiovascular pharmacology.

[101]  M. Yano,et al.  A novel endothelin ETA receptor antagonist, BQ-485, and its preventive effect on experimental cerebral vasospasm in dogs. , 1993, Biochemical and biophysical research communications.

[102]  D. Mann,et al.  Hemodynamic Effects of Tezosentan, an Intravenous Dual Endothelin Receptor Antagonist, in Patients With Class III to IV Congestive Heart Failure , 2001, Circulation.

[103]  B. Vollrath,et al.  The polycationic aminoglycosides modulate the vasoconstrictive effects of endothelin: relevance to cerebral vasospasm , 2001, British journal of pharmacology.

[104]  Y. Notsu,et al.  An endothelin ETA receptor antagonist, FR139317, ameliorates cerebral vasospasm in dogs. , 1993, Life sciences.