Endothelin antagonists

Lancet

Volumn 353, Issue 9147, 1999, Pages 133-138

  Benigni, Ariela ^a   Remuzzi, Giuseppe ^a  

^a MARIO NEGRI INST PHARMACOL RES   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

2 [[2 [[2 [[(HEXAHYDRO 1H AZEPIN 1 YL)CARBONYL]AMINO] 4 METHYLPENTANOYL]AMINO] 3 (1 METHYL 1H INDOL 3 YL)PROPIONYL]AMINO] 3 (2 PYRIDYL)PROPIONIC ACID; 3 (2 CARBOXYMETHOXY 4 METHOXYPHENYL) 1 (3,4 METHYLENEDIOXYPHENYL) 5 PROPOXY 2 INDANCARBOXYLIC ACID; 3 BENZYL 4 (4 METHOXYPHENYL) 2 (3,4 METHYLENEDIOXYPHENYL) 4 OXO 2 BUTENOIC ACID; 4 (4 METHOXYPHENYL) 2 (3,4 METHYLENEDIOXYPHENYL) 4 OXO 3 (3,4,5 TRIMETHOXYBENZYL) 2 BUTENOIC ACID; 4 TERT BUTYL N [6 (2 HYDROXYETHOXY) 5 (3 METHOXYPHENOXY) 4 PYRIMIDINYL]BENZENESULFONAMIDE; 5 DIMETHYLAMINO N (3,4 DIMETHYL 5 ISOXAZOLYL) 1 NAPHTHALENESULFONAMIDE; ATRASENTAN; BOSENTAN; BQ 610; CP 170687; CYCLO(DEXTRO TRYPTOPHYL DEXTRO ASPARTYLPROLYL DEXTRO VALYLLEUCYL); DARUSENTAN; ENDOTHELIN; ENDOTHELIN 1; ENDOTHELIN 1 [11-21]; ENDOTHELIN 2; ENDOTHELIN 3; ENDOTHELIN A RECEPTOR ANTAGONIST; ENDOTHELIN B RECEPTOR ANTAGONIST; ENDOTHELIN RECEPTOR; ENDOTHELIN RECEPTOR ANTAGONIST; ENRASENTAN; L 751281; L 754142; N (2,6 DIMETHYLPIPERIDINOCARBONYL) 4 METHYLLEUCYL DEXTRO (1 METHOXYCARBONYLTRYPTOPHANYL) DEXTRO NORLEUCINE; N ACETYL 10,11 DIHYDRO 5H DIBENZO[A,D]CYCLOHEPTEN 5 YLGLYCYLLEUCYLASPARTYLISOLEUCYLISOLEUCYLTRYPTOPHAN; N ACETYL 3,3 DIPHENYL DEXTRO ALANYLLEUCYLASPARTYLISOLEUCYLISOLEUCYLTRYPTOPHAN; PERHYDRO 1 AZEPINYLCARBONYLLEUCYL DEXTRO TRYPTOPHYL DEXTRO TRYPTOPHAN; TAK 044; UNCLASSIFIED DRUG; VASOCONSTRICTOR AGENT;

CEREBROVASCULAR DISEASE; CLINICAL TRIAL; HEART FAILURE; HEART INFARCTION; HUMAN; HYPERTENSION; KIDNEY DISEASE; NONHUMAN; PATHOPHYSIOLOGY; PRIORITY JOURNAL; PULMONARY HYPERTENSION; REVIEW;

EID: 0033537345     PISSN: 01406736     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0140-6736(98)09423-9     Document Type: Review

References (87)

1. Yanagisawa M, Kurihara H, Kimura Set al. A novel potent vasoconstrictor peptide produced by vascular endothelial cells. Nature. 332:1988;411-415.
2. Inoue A, Yanagisawa M, Kimura Set al. The human endothelin family: three structurally and pharmacologically distinct isopeptides predicted by three separate genes. Proc Natl Acad Sci USA. 86:1989;2863-2867.
3. Remuzzi G, Benigni A Endothelins in the control of cardiovascular and renal function. Lancet. 342:1993;589-593.
4. Moreland S, McMullen DM, Delaney CL, Lee VG, Hunt JT Venous smooth muscle contains vasoconstrictor ETB-like receptors. Biochem Biophys Res Commun. 184:1992;100-106.
5. Iwasaki S, Homma T, Matsuda Y, Kon V Endothelin receptor subtype B mediates autoinduction of endothelin-1 in rat mesangial cells. J Biol Chem. 270:1995;6997-7003.
6. Benigni A Defining the role of endothelins in renal pathophysiology on the basis of selective and unselective endothelin receptor antagonist studies. Curr Opin Nephrol Hypertens. 4:1995;349-353.
7. Pollock DM, Opgenorth TJ Evidence for endothelin-induced renal vasoconstriction independent of ETA receptor activation. Am J Physiol. 264:1993;R222-226.
8. Benigni A, Remuzzi G Endothelin receptor antagonists: which are the therapeutic perspectives in renal diseases? Nephrol Dial Transplant. 13:1998;5-7.
9. Sorensen SS, Madsen JK, Pedersen EB Systemic and renal effect of intravenous infusion of endothelin-1 in healthy human volunteers. Am J Physiol. 266:1994;F411-418.
10. Nishikibe M, Tsuchida S, Okada Met al. Antihypertensive effects of a newly synthesized endothelin antagonist, BQ 123, in a genetic hypertensive model. Life Sci. 52:1993;717-724.
11. Douglas SA, Gellai M, Ezekial M, Feuerstein GZ, Elliot JD, Ohlstein EH Antihypertensive actions of the novel nonpeptide endothelin receptor antagonist SB 209670. Hypertension. 25:1995;818-822.
12. Schiffrin EL, Turgeon A, Deng LY Effect of chronic ETA-selective endothelin receptor antagonism on blood pressure in experimental and genetic hypertension in rats. Br J Pharmacol. 121:1997;935-940.
13. Barton M, d'Uscio LV, Shaw S, Meyer P, Moreau P, Luscher TF ET(A) receptor blockade prevents increased tissue endothelin-1, vascular hypertrophy, and endothelial dysfunction in salt-sensitive hypertension. Hypertension. 31:1998;499-504.
14. Yu M, Gopalakrishnan V, McNeill JR. Hemodynamic effects of a selective endothelin-A receptor antagonist in deoxycorticosterone acetate-salt hypertensive rats. J Cardiovasc Pharmacol 1998; 31 (suppl 1): S262-64.
15. Sharifi AM, Schiffrin EL Apoptosis in aorta of deoxycorticosterone acetate-salt hypertensive rats: effect of endothelin receptor antagonism. J Hypertens. 15:1997;1441-1448.
16. Kurihara Y, Kurihara H, Suzuki Het al. Elevated blood pressure and craniofacial abnormalities in mice deficient in endothelin-1. Nature. 368:1994;703-710.
17. Niranjan V, Télémaque S, de Wit D, Gerard RD, Yanagisawa M Systemic hypertension induced by hepatic overexpression of human preproendothelin-1 in rats. J Clin Invest. 98:1996;2364-2372.
18. Yokokawa K, Tahara H, Kohno Met al. Hypertension associated with endothelin-secreting malignant hemangioendothelioma. Ann Intern Med. 114:1991;213-215.
19. Saito Y, Nakao K, Mukoyama M, Imura H Increased plasma endothelin level in patients with essential hypertension. N Engl J Med. 322:1990;205.
20. Lerman A, Edwards BS, Hallett JW, Heublein DM, Sandberg SM, Burnett JC Circulating and tissue endothelin immunoreactivity in advanced atherosclerosis. N Engl J Med. 325:1991;997-1001.
21. Ohlstein EH, Arleth A, Bryan H, Elliott JD, Po Sung C The selective endothelin ETA receptor antagonist BQ123 antagonizes endothelin-1-mediated mitogenesis. Eur J Pharmacol. 225:1992;347-350.
22. Douglas SA, Louden C, Vickery Clark LMet al. A role for endogenous endothelin-1 in neointimal formation after rat carotid artery balloon angioplasty: protective effects of the novel nonpeptide endothelin receptor antagonist SB 209670. Circ Res. 75:1994;190-197.
23. Okada K, Nishida Y, Murakami Het al. Role of endogenous endothelin in the development of graft arteriosclerosis in rat cardiac allografts: antiproliferative effects of bosentan, a nonselective endothelin receptor antagonist. Circulation. 97:1998;2346-2351.
24. Sakai S, Miyauchi T, Kobayashi M, Yamaguchi I, Goto K, Sugishita Y Inhibition of myocardial endothelin pathway improves long-term survival in heart failure. Nature. 384:1996;353-355.
25. Spinale FG, Walker JD, Murkherjee R, Iannini JP, Keever AT, Galagher KP Concomitant endothelin receptor subtype-A blockade during the progression of pacing induced congestive heart failure in rabbits: beneficial effects on left ventricular and myocyte function. Circulation. 95:1997;1918-1929.
26. Teerlink JR, Loffler BM, Hess P, Marie JP, Clozel M, Clozel JP Role of endothelin in the maintenance of blood pressure in conscious rats with chronic heart failure. Acute effects of the endothelin receptor antagonist Ro 47-0203 (bosentan). Circulation. 9:1994;2510-2518.
27. McMurray JJ, Ray SG, Abdullah I, Dargie HJ, Morton JJ Plasma endothelin in chronic heart failure. Circulation. 85:1992;1374-1379.
28. Rodenheffer RJ, Lerman A, Heublein DM, Burnett JJ Increased plasma concentrations of endothelin in congestive heart failure in humans. Mayo Clin Proc. 67:1992;719-724.
29. Wei CM, Lerman A, Rodhaffer RJet al. Endothelin in human congestive heart failure. Circulation. 89:1994;1580-1586.
30. Sakai S, Miyauchi T, Sakurai T Endogenous endothelin-1 participates in the maintenance of cardiac function in rats with congestive heart failure: marked increases in endothelin-1 production in the failing heart. Circulation. 93:1996;1214-1222.
31. Mulder P, Richard V, Derumeaux Get al. Role of endogenous endothelin in chronic heart failure. Effect of long-term tratment with an endothelin antagonist on survival, hemodynamics, and cardiac remodelling. Circulation. 96:1997;1976-1982.
32. Fraccarollo D, Hu K, Galuppo P, Gaudron P, Ertl G Chronic endothelin receptor blockade attenuates progressive ventricular dilation and improves cardiac function in rats with myocardial infarction: possible involvement of myocardial endothelin system in ventricular remodeling. Circulation. 96:1997;3963-3973.
33. Miyauchi T, Yanagisawa M, Tomizawa Tet al. Increased plasma concentrations in endothelin-1 and big endothelin-1 in acute myocardial infarction. Lancet. i:1989;53-54.
34. Pacher R, Stanek B, Hulsmann Met al. Prognostic impact of big endothelin-1 plasma concentrations compared with invasive hemodynamic evaluation in severe heart failure. J Am Coll Cardiol. 27:1996;633-641.
35. Prie S, Leung TK, Cernacek P, Ryan JW, Dupuis J The orally active ET(A) receptor antagonist (+)-(S)-2-(4,6-dimethoxy-pyrimidin-2-oxloxy)-3 -methoxy-3,3-diphenyl-propionic acid (LU 135252) prevents the development of pulmonary hypertension and endothelial metabolic dysfunction in monocrotaline-treated rats. J Pharmacol Exp Ther. 282:1997;1312-1318.
36. Chen SJ, Chen YF, Opgenorth TJet al. The orally active nonpeptide endothelin-A-receptor antagonist A-127722 prevents and reverses hypoxia-induced pulmonary hypertension and pulmonary vascular remodelling in Sprague-Dawley rats. J Cardiovasc Pharmacol. 29:1997;713-725.
37. DiCarlo VS, Chen SJ, Meng QCet al. ETA-receptor antagonist prevents and reserves chronic hypoxia-induced pulmonary hypertension in rat. Am J Physiol. 269:1995;L690-697.
38. Willette RN, Ohlstein EH, Mitchell MPet al. Nonpeptide endothelin receptor antagonists. VIII: attenuation of acute hypoxia-induced pulmonary hypertension in the dog. J Pharmacol Exp Ther. 280:1997;695-701.
39. Ferro C, Webb D The clinical potential of endothelin receptor antagonists in cardiovascular medicine. Drugs. 51:1996;12-27.
40. Stewart D, Levey R, Cernacek Pet al. Increased plasma endothelin-1 in pulmonary hypertension: marker or mediator of disease? Ann Intern Med. 114:1991;464-469.
41. Giaid A, Yanagisawa M, Langleben Det al. Expression of endothelin-1 in the lungs of patients with pulmonary hypertension. N Engl J Med. 328:1993;1732-1739.
42. Itoh S, Sasaki T, Ide Ket al. A novel endothelin ETA receptor antagonist BQ 485 and its preventive effect on experimental cerebral vasospasm in dogs. Biochem Biophys Res Commun. 195:1993;969-975.
43. Willette RN, Zhang H, Mitchell MPet al. Non peptide endothelin antagonist: cerebrovascular characterization and effects on delayed cerebral vasospasm. Stroke. 25:1994;2450-2456.
44. Brooks DP, DePalma PD, Gellai Met al. Nonpeptide endothelin receptor antagonists. III. Effect of SB 209670 and BQ123 on acute renal failure in anesthetized dogs. J Pharmacol Exp Ther. 271:1994;1-7.
45. Stingo AJ, Clavell AL, Aarhus LL, Burnett JC Jr. Biological role for the endothelin-A receptor in aortic cross-clamping. Hypertension. 22:1993;62-66.
46. Buyukgebiz O, Aktan AO, Haklar Get al. BQ-123, a specific endothelin (ETA) receptor antagonist, prevents ischemia-reperfusion injury in kidney transplantation. Transplant Int. 9:1996;201-207.
47. Herrero I, Torras J, Riera M, et al. Prevention of cold ischemia-reperfusion injury by an endothelin receptor antagonist in experimental renal transplantation. J Am Soc Nephrol 1997; 8: 657A (abstr).
48. Perico N, Dadan J, Remuzzi G Endothelin mediates the renal vasoconstriction induced by cyclosporine in the rat. J Am Soc Nephrol. 1:1990;76-83.
49. Brooks DP, Contino LC Prevention of cyclosporine A-induced renal vasoconstriction by the endothelin receptor antagonist SB 209670. Eur J Pharmacol. 294:1995;571-576.
50. Kon V, Hunley TE, Fogo A Combined antagonism of endothelinA/B receptors links endothelin to vasoconstriction whereas angiotensin II affects fibrosis. Transplantation. 60:1995;89-95.
51. Benigni A, Perico N, Ladny Jet al. Increased urinary excretion of endothelin-1 and its precursor, big-endothelin, in rats chronically treated with cyclosporine. Transplantation. 52:1990;175-177.
52. Bird E, Giancarli M, Burton D, Durham S. Endothelin-A receptors mediate ET effects in radiocontrast nephropathy. J Am Soc Nephrol 1995; 6: 994 (abstr).
53. Pollock DM, Polakowski JS. Beneficial effect of ETA receptor blockade in radiocontrast-induced nephropathy in the rat. J Am Soc Nephrol 1995; 6: 667 (abstr).
54. Oldroyd SD, Haylor JL, Morcos SK Bosentan, an orally active endothelin antagonist: effect on the renal response to contrast media. Radiology. 196:1995;661-665.
55. Karam H, Burneval P, Clozel J, Loffler B, Bariety J, Clozel M Role of endothelin in acute renal failure due to rhabdomyolysis in rats. J Pharm Exp Ther. 274:1995;481-486.
56. Hocher B, Thone-Reineke C, Rohmeiss Pet al. Endothelin-1 transgenic mice develop glomerulosclerosis, interstitial fibrosis, and renal cysts but not hypertension. J Clin Invest. 99:1997;1380-1389.
57. Liefeldt L, Bocker W, Schonfelder G, Zintz M, Paul M Regulation of the endothelin system in transgenic rats expressing the human endothelin-2 gene. J Cardiovasc Pharmacol. 26:1995;S32-35.
58. Benigni A, Zoja C, Corna Det al. A specific endothelin subtype A receptor antagonist protects against injury in renal disease progression. Kidney Int. 44:1993;440-444.
59. Benigni A, Zoja C, Corna Det al. Blocking both type A and B endothelin receptors in the kidney attenuates renal injury and prolongs survival in rats with remnant kidney. Am J Kidney Dis. 27:1996;416-423.
60. Nabokov A, Amann K, Wagner J, Gehlen F, Munter K, Ritz E Influence of specific and non-specific endothelin receptor antagonists on renal morphology in rats with surgical renal ablation. Nephrol Dial Transplant. 11:1996;514-520.
61. Nakamura T, Ebihara I, Tomino Y, Koide H Effect of a specific endothelin A receptor antagonist on murine lupus nephritis. Kidney Int. 47:1995;481-489.
62. Benigni A, Colosio V, Brena C, Bruzzi I, Bertani T, Remuzzi G Unselective inhibition of endothelin receptors reduces renal dysfunction in experimental diabetes. Diabetes. 47:1998;450-456.
63. Ihara M, Noguchi K, Saeki Tet al. Biological profiles of highly potent novel endothelin antagonists for the ETA receptor. Life Sci. 50:1992;247-255.
64. Ishikawa K, Ihara M, Noguchi Ket al. Biochemical and pharmacological of a potent and selective endothelin-B receptor antagonist BQ788. Proc Natl Acad Sci USA. 91:1994;4892-4896.
65. Clozel M, Breu V, Gray GAet al. Pharmacological characterization of bosentan, a new potent orally active nonpeptide endothelin receptor antagonist. J Pharmacol Exp Ther. 270:1994;228-235.
66. Cody WL, Doherty AM, He JXet al. The rational design of a highly potent combined ETA and ETB receptor antagonist (PD 145065) and related analogues. Med Chem Res. 3:1993;154-162.
67. Haynes WG, Webb DJ Contribution of endogenous generation of endothelin-1 to basal vascular tone. Lancet. 344:1994;852-854.
68. Haynes WG, Ferro CJ, O'Kane KPJ, Somerville D, Lomax CC, Webb DJ Systemic endothelin receptor blockade decreases peripheral vascular resistance and blood pressure in humans. Circulation. 93:1996;1860-1870.
69. Love MP, Haynes WG, Gray GA, Webb DJ, McMurray JJV Vasodilator effects of endothelin-converting enzyme inhibition and ETA receptor blockade in chronic heart failure patients treated with ACE inhibitors. Circulation. 94:1996;2131-2137.
70. Kiowski W, Sutsch G, Huniziker Pet al. Evidence for endothelin-1 mediated vasoconstriction in severe chronic heart failure. Lancet. 346:1995;732-736.
71. Krum H, Viskoper RJ, Lacourciere Y, Budde M, Charlon V, for the Bosentan Hypertension Investigators. The effect of an endothelin-receptor antagonist, bosentan, on blood pressure in patients with essential hypertension. N Engl J Med 1998; 338: 784-90.
72. Haynes WG, Ferro CJ, Webb DJ Bosentan in essential hypertension. N Engl J Med. 339:1998;346.
73. Patel TR Therapeutic potential of endothelin receptor antagonists in cerebrovascular disease. CNS Drugs. 5:1996;293-310.
74. Binet I, Wallnofer A, Weber C, Jones R, Thiel G. Renal hemodynamics and pharmacokinetics of bosentan with and without cyclosporine A. Nephrol Dial Transplant (in press).
75. Wang A, Bashore T, Holcslaw T, et al. Randomized prospective double blind multicentre trial of endothelin receptor antagonist in the prevention of contrast nephrotoxicity. J Am Soc Nephrol 1998; 9: 137A (abstr).
76. Benigni A, Remuzzi G The renoprotective potential of endothelin receptor antagonists. Exp Opin Ther Patents. 7:1997;139-149.
77. Kurihara Y, Kurihara H, Oda Het al. Aortic arch malformations and ventricular septal defect in mice deficient in endothelin-1. J Clin Invest. 96:1995;293-300.
78. Clouthier DE, Hosoda K, Richardson JAet al. Cranial and cardiac neural crest defect in endothelin-A receptor-deficient mice. Development. 125:1998;813-824.
79. Hosada K, Hammer E, Richardson Jet al. Targeted and natural (piebald-lethal) mutations of endothelin B receptor gene produce megacolon associated with spotted coat color in mice. Cell. 79:1994;1267-1276.
80. Hofstra RMW, Osinga J, Tan-Sindhunata Get al. A homozygous mutation in the endothelin-3 gene associated with a combined Waardenburg type 2 and Hirschsprung phenotype (Shah-Waardenburg syndrome). Nat Genet. 12:1996;445-447.
81. Puffenberger EG, Hosoda K, Washington SSet al. A missense mutation of the endothelin-B receptor gene in multigenetic Hirschsprung's disease. Cell. 79:1994;1257-1266.
82. Lopez-Farre A, Gomez-Garre D, Bernabeu F, Lopez Novoa JM A role for endothelin in the maintenance of post-ischaemic renal failure in the rat. J Physiol. 444:1991;513-522.
83. Mino N, Kobayash M, Nakijima Aet al. Protective effect of a selective endothelin receptor antagonist, BQ123, in ischemic acute renal failure in rats. Eur J Pharmacol. 221:1992;77-83.
84. Kusumoto K, Kubo K, Kandori Het al. Effects of a new endothelin antagonist, TAK-044, on post-ischemic acute renal failure in rats. Lif Sci. 55:1994;301-310.
85. Clozel M, Breu V, Burri Ket al. Pathophysiological role of endothelin revealed by the first orally active endothelin receptor antagonist. Nature. 365:1993;759-761.
86. Gellai M, Jugus M, Fletcher T, De Wolf R, Nambi P Reversal of post-ischemic acute renal failure with a selective endothelin A receptor antagonist in the rat. J Clin Invest. 93:1994;900-906.
87. Gellai M, Jugus M, Fletcher T, et al. The endothelin receptor antagonist (±)-SB 209670, reverses ischemia-induced acute renal failure (ARF) in the rat. Fed Am Soc Exp Biol J 1994; 8: A260 (abstr).