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

Neurosurgery

Volumn 43, Issue 6, 1998, Pages 1409-1418

  Wanebo, John E ^a,b   Arthur, Adam S ^c   Louis, Hunter G ^c   West, Kim ^c   Kassell, Neal F ^c   Lee, Kevin S ^c   Helm, Gregory A ^c  

^a WALTER REED ARMY MEDICAL CENTER   (United States)

^b WASHINGTON UNIVERSITY SCHOOL OF MEDICINE   (United States)

^c UNIVERSITY OF VIRGINIA   (United States)

Author keywords

Cerebral vasospasm; Endothelin receptor; Endothelin 1; Subarachnoid hemorrhage

Indexed keywords

ENDOTHELIN A RECEPTOR ANTAGONIST; SITAXSENTAN; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BASILAR ARTERY; BRAIN VASOSPASM; CONTROLLED STUDY; INTRAVENOUS DRUG ADMINISTRATION; MALE; MEAN ARTERIAL PRESSURE; NONHUMAN; PRIORITY JOURNAL; RABBIT; SUBARACHNOID HEMORRHAGE;

EID: 0031760395     PISSN: 0148396X     EISSN: None     Source Type: Journal    
DOI: 10.1097/00006123-199812000-00086     Document Type: Article

References (95)

1. Alafaci C, Salpietro FM, Iacopino DC, Edvinsson L, Tomasello F: Endothelin: An endothelium-derived vasoactive peptide and its possible role in the pathogenesis of cerebral vasospasm. Ital J Neurol Sci 12[Suppl 11]:55-58, 1991.
2. Arai H, Hori S, Aramori I, Ohkubo H, Nakanishi S: Cloning and expression of a cDNA encoding an endothelin receptor. Nature 348:730-732, 1990.
3. Arinami T, Ishikawa M, Inoue A, Yanagisawa M, Masaki T, Yoshida MC, Hamaguchi H: Chromosomal assignments of the human endothelin family genes: The endothelin-1 gene (EDN1) to 6p23-p24, the endothelin-2 gene (EDN2) to 1p34, and the endothelin-3 gene (EDN3) to 20q13.2-q13.3. Am J Hum Genet 48:990-996, 1991.
4. Asano T, Ikegaki I, Satoh S, Suzuki Y, Shibuya M, Sugita K, Hidaka H: Endothelin: A potential modulator of cerebral vasospasm. Eur J Pharmacol 190:365-372, 1990.
5. Asano T, Ikegaki I, Suzuki Y, Satoh S, Shibuya M: Endothelin and the production of cerebral vasospasm in dogs. Biochem Biophys Res Commun 159:1345-1351, 1989.
6. Bacic F, Uematsu S, McCarron RM, Spatz M: Secretion of immunoreactive endothelin-1 by capillary and microvascular endothelium of human brain. Neurochem Res 17:699-702, 1992.
7. Caner HH, Kwan AL, Arthur AS, Jeng A, Kassell NF, Lee KS: Systemic administration of an inhibitor of endothelin converting enzyme attenuates cerebral vasospasm following experimental subarachnoid hemorrhage. J Neurosurg 85:917-922, 1996.
8. A receptor antagonist, prevents the early cerebral vasospasm following subarachnoid hemorrhage after intracisternal but not intravenous injection. Life Sci 52:825-834, 1993.
9. Clozel M, Breu V, Burri K, Cassai JM, Fischil W, Gray GA, Hirth G, Loffler BM, Miller M, Neidhart W, Ramuz H: Pathophysiological role of endothelin revealed by the first orally active endothelin receptor antagonist. Nature 356:759-761, 1993.
10. Cocks TM, Malta E, King SJ, Woods RL, Angus JA: Oxyhaemoglobin increases the production of endothelin-1 by endothelial cells in culture. Eur J Pharmacol 196:177-182, 1991.
11. Cosentino F, Katusic ZS: Does endothelin-1 play a role in the pathogenesis of cerebral vasospasm? Stroke 25:904-908, 1994.
12. A-receptor antagonist BQ-123 and phosphoramidon on cerebral vasospasm. J Cardiovasc Pharmacol 22[Suppl 8]:S332-S335, 1993.
13. Delgado TJ, Arbab MAR, Warburg J, Svendgaard NA: The role of vasopressin in acute cerebral vasospasm: Effect on spasm of a vasopressin antagonist or vasopressin antiserum. J Neurosurg 68:266-273, 1988.
14. Doherty AM: Endothelin: A new challenge. J Med Chem 35:1493-1508, 1992.
15. Ehrenreich H, Schilling L: New developments on the understanding of cerebral vasoregulation and vasospasm: The endothelin nitric oxide network. Clev Clin J Med 62:105-116, 1995.
16. Ehrenreich H, Anderson RW, Ogino Y, Rieckmann P, Costa T, Wood GP, Coligam JE, Kehrl JH, Fauci AS: Selective autoregulation of endothelins in primary astrocyte cultures: Endothelin receptor-mediated potentiation of endothelin-1 secretion. New Biol 2:135-141, 1991.
17. Ehrenreich H, Lange M, Near KA, Anneser F, Schoeller LAC, Schmid R, Winkler PA, Kehrl JH, Schmiedek P, Goebel FD: Long term monitoring of immunoreactive endothelin-1 and endothelin-3 in ventricular cerebrospinal fluid, plasma, and 24-h urine of patients with subarachnoid hemorrhage. Res Exp Med (Berl) 192:257-268, 1992.
18. Emori T, Hirata Y, Marund E: Specific receptors for endothelin-3 in bovine endothelial cells and its cellular mechanisms of action. FEBS Lett 263:261-264, 1990.
19. Faraci FM: Effects of endothelin and vasopressin on cerebral blood vessels. Am J Physiol 257:H799-H803, 1992.
20. Feger GI, Schilling L, Ehrenreich H, Wahl M: Endothelin-induced contraction and relaxation in rat isolated basilar artery: Effect of BQ 123. J Cereb Blood Flow Metab 14:845-852, 1994.
21. Foley PL, Caner HH, Kassell NF, Lee KS: Reversal of subarachnoid hemorrhage-induced vasoconstriction with an endothelin receptor antagonist. Neurosurgery 34:108-113, 1994.
22. Foley PL, Kassell NF, Hudson SB, Lee KS: Hemoglobin penetration in the wall of the rabbit basilar artery after subarachnoid hemorrhage and intracisternal hemoglobin injection. Acta Neurochir (Wien) 123:82-86, 1993.
23. Fujimori A, Yanagisawa M, Saito A, Goto K, Masaki T, Mima T, Takakura K, Shigeno T: Endothelin in plasma and cerebrospinal fluid of patients with subarachnoid haemorrhage. Lancet 336:633, 1990 (letter).
24. Fujiwara S, Kassell NF, Sasaki T, Nakagomi T, Lehman RM: Selective hemoglobin inhibition of endothelin-dependent vasodilation of rabbit basilar artery. J Neurosurg 64:445-452, 1986.
25. Gaetani P, Rodriguez Y, Baena R, Grignani G, Spanu G, Pacchiarini L, Paoletti P: Endothelin and aneurysmal subarachnoid hemorrhage: A study of subarachnoid cisternal cerebrospinal fluid. J Neurol Neurosurg Psychiatry 57:66-72, 1994.
26. Gavras H, Andrews P, Papadopoulos N: Reversal of experimental delayed cerebral vasospasm by angiotensin-converting enzyme inhibition. J Neurosurg 55:884-888, 1981.
27. Giaid A, Gibson SJ, Ibrahim NBN, Legon S, Bloom SR, Yanagisawa M, Masaki T, Varndell IM, Polak JM: Endothelin-1, an endothelin-derived peptide, is expressed in neurons of the human spinal cord and dorsal root ganglia. Proc Natl Acad Sci USA 86:7634-7638, 1989.
28. Greenberg DA, Chan H, Sampson HA: Endothelins and the nervous system. Neurology 42:25-31, 1992.
29. Hardebo JE, Kahrstrom J, Owman C, Salford LG: Endothelin is a potent constrictor of human intracranial arteries and veins. Blood Vessels 26:249-253, 1989.
30. Hino A, Weir BKA, Macdonald RL, Trusted RA, Kim CJ, Johns LM: Prospective, randomized, double-blind trial of BQ-123 and bosentan for prevention of vasospasm following subarachnoid hemorrhage in monkeys. J Neurosurg 83:503-509, 1995.
31. Hongo K, Kassell NF, Nakagomi T, Sasaki T, Tsukahara T, Ogawa H, Vollmer DG, Lehman RM: Subarachnoid hemorrhage inhibition of endothelin-derived relaxing factor in rabbit basilar artery. J Neurosurg 69:247-253, 1988.
32. Ide K, Yamakawa K, Nakagomi T, Sasaki T, Saito I, Kurihara H, Yosizami M, Takakura K: The role of endothelin in the pathogenesis of vasospasm following subarachnoid hemorrhage. Neurol Res 11:101-104, 1989.
33. Inoue A, Yanagisawa M, Kimura S, Kasuya Y, Miyauchi T, Goto K, Masaki T: The human endothelin family: Three structurally and pharmacologically distinct isopeptides by three separate genes. Proc Natl Acad Sci U S A 86:2863-2867, 1989.
34. A receptor mRNA expression in a canine subarachnoid hemorrhage model. J Neurosurg 81:759-764, 1994.
35. A receptor antagonist, BQ-485, and its preventive effect on experimental cerebral vasospasm in dogs. Biochem Biophys Res Commun 195:969-975, 1993.
36. Jansen I, Fallgren B, Edvinsson L: Mechanisms of action of endothelin on isolated feline cerebral arteries: In vitro pharmacology and electrophysiology. J Cereb Blood Flow Metab 9:743-747, 1989.
37. Johshita H, Kassell NF, Sasaki T, Nakagomi T, Ogawa H: Biphasic constriction of rabbit basilar artery following experimental subarachnoid hemorrhage: A morphometric study. Surg Neurol 37: 106-114, 1992.
38. Kassell NF, Torner JC: The International Cooperative Study on timing of aneurysm surgery: An update. Stroke 15:566-570, 1984.
39. Kassell NF, Sasaki T, Colohan ART, Nazar G: Cerebral vasospasm following aneurysmal subarachnoid hemorrhage. Stroke 16:562-572, 1985.
40. Kasuya H, Weir BK, White DM, Stefansson K: Mechanism of oxyhemoglobin-induced release of endothelin-1 from cultured vascular endothelial cells and smooth-muscle cells. J Neurosurg 79:892-898, 1993.
41. Kobayashi H, Hayashi M, Kobayashi S, Kabuto M, Handa Y, Kawano H: Effect of endothelin on the canine basilar artery. Neurosurgery 27:357-361, 1990.
42. Kobayashi H, Hayashi M, Kobayashi S, Kabuto M, Handa Y, Kawano H, Ide H: Cerebral vasospasm and vasoconstriction caused by endothelin. Neurosurgery 28:673-678, 1991.
43. Kraus GE, Bucholz RD, Yoon KW, Knuepfer MM, Smith KR: Cerebrospinal fluid endothelin-1 and endothelin-3 level in normal and neurosurgical patients: A clinical study and literature review. Surg Neurol 35:20-29, 1991.
44. Kwan AL, Bavbek M, Jeng AY, Maniara W, Toyoda T, Lappe RW, Kassell NF, Lee KS: Prevention and reversal of cerebral vasospasm by an endothelin-converting enzyme inhibitor (CG 26303) in an experimental model of subarachnoid hemorrhage. J Neurosurg 87:281-286, 1997.
45. Lee ME, de la Monte SM, Ng SC, Block KD: Expression of the potent vasoconstrictor endothelin in human central nervous system. J Clin Invest 86:141-147, 1990.
46. Lehman RM, Kassell NF, Nazar GB, Weir BK, Johshita H, Nosko M, Duling BR, Owens GK: Morphometric methods in the study of vasospasm, in Wilkins R (ed): Cerebral Vasospasm, New York, Raven Press, 1988, pp 113-118.
47. Lin HY, Kaji EH, Winkel GK, Ives HE, Lodish HF: Cloning and functional expression of vascular smooth muscle endothelin-1 receptor. Proc Natl Acad Sci U S A 88:3185-3189, 1991.
48. MacCumber MW, Ross CA, Snyder SH: Endothelin in brain: Receptors, mitogenesis, and biosynthesis in glial cells. Proc Natl Acad Sci U S A 87:2359-2363, 1990.
49. Macdonald RL, Weir BKA: A review of hemoglobin and the pathogenesis of cerebral vasospasm. Stroke 22:971-982, 1991.
50. Maggi CA, Giuliani S, Patacchini R, Rovero P, Giachetti A, Meli A: The activation of peptides of the endothelin family in various mammalian smooth muscle preparations. Eur J Pharmacol 174: 23-31, 1989.
51. Martin de Aguilera E, Irurzun A, Vila JM, Aldosoro M, Galeote MS, Lhich S: Role of endothelium and calcium channels in endothelin-induced contraction of human cerebral arteries. Br J Pharmacol 99:439-440, 1990.
52. Masaoka H, Suzuki R, Hirata Y, Emori T, Marumo F, Hirakawa K: Raised plasma endothelin in aneurysmal subarachnoid hemorrhage. Lancet 2:1402, 1989 (letter).
53. Matsumura Y, Ikegawa R, Suzuki Y, Takaoka M, Uchida T, Kido H, Shinyama H, Hayashi K, Watanabe M, Morimoto S: Phosphoramidon prevents cerebral vasospasm following subarachnoid hemorrhage in dog: The relationship to endothelin-1 levels in the cerebrospinal fluid. Life Sci 49:841-848, 1991.
54. Mima T, Yanagisawa M, Shigeno T, Saito A, Goto K, Takakura K, Masaki T: Endothelin acts in feline and canine cerebral arteries from the adventitial side. Stroke 20:1553-1556, 1989.
55. Nakagomi T, Kassell NF, Hongo K, Sasaki T: Pharmacological reversibility of experimental cerebral vasospasm. Neurosurgery 27:582-586, 1990.
56. Nakagomi T, Kassell NF, Sasaki T, Lehman RM, Hongo K, Ogawa H, Vollmer DG: Time course of the blood-arterial wall barrier disruption following experimental subarachnoid haemorrhage. Acta Neurochir (Wien) 98:176-183, 1989.
57. A receptor antagonist, FR139317, ameliorates cerebral vasospasm in dogs. Life Sci 52:1869-1874, 1993.
58. Ohlstein EH, Storer BL: Oxyhemoglobin stimulation of endothelin production in cultured cells. J Neurosurg 77:274-278, 1992.
59. Onoda K, Ono S, Ogihara K, Shiota T, Asari S, Ohmoto T, Ninomiya Y: Inhibition of vascular construction by intracisternal administration of preproendothelin-1 mRNA antisense oligoDNA in rat experimental vasospasm model. J Neurosurg 85:846-852, 1996.
60. Opgenorth TJ: Endothelin receptor antagonism, in August JT, Anders MW, Murad F, Coyle JT (eds): Advances in Pharmacology. San Diego, Academic Press, 1995, vol 33, pp 1-65.
61. Papadopoulos SM, Gilbert LL, Webb RC, D'Amato CJ: Characterization of contractile responses to endothelin in human cerebral arteries: Implications for cerebral vasospasm. Neurosurgery 26: 810-815, 1990.
62. Pluta RM, Boock RJ, Afshar JK, Clouse K, Bacic M, Ehrenreich H, Oldfield EH: Source and cause of endothelin-1 release into cerebrospinal fluid after subarachnoid hemorrhage. J Neurosurg 87: 287-293, 1997.
63. Robinson MJ, McCulloch J: Contractile responses to endothelin in feline cortical vessels in situ. J Cereb Blood Flow Metab 10:285-295, 1990.
64. Roux S, Loffler BM, Gray GA, Sprecher U, Clozel M, Clozel JP: The role of endothelin in experimental cerebral vasospasm. Neurosurgery 37:78-85, 1995.
65. Rubanyi GM, Polokoff MA: Endothelins: Molecular biology, biochemistry, pharmacology, physiology, and pathophysiology. Pharmacol Rev 46:325-415, 1994.
66. Sahs AL, Nibbelink DW, Torner JC (eds): Aneurysmal Subarachnoid Hemorrhage: Report of the Cooperative Study. Baltimore, Urban & Swartzenberg, 1981.
67. Saito A, Shiba R, Kimura S, Yanagisawa M, Goto K, Masaki T: Vasoconstrictor response of large cerebral arteries of cat to endothelin, an endothelium-derived vasoactive peptide. Eur J Pharmacol 162:353-358, 1989.
68. Saito A, Shiba R, Yanagisawa M, Masaki T, Kimura S, Yamada K, Mima T, Shigeno T, Goto K: Endothelin: Vasoconstrictor effects and localization in canine cerebral arteries. Br J Pharmacol 63: 1129-1135, 1991.
69. Sakurai T, Yanagisawa M, Takuwa Y, Miyazaki H, Kimura S, Goto K, Masaki T: Cloning of cDNA encoding a non-isopeptide-selection subtype of the endothelin receptor. Nature 348:732-735, 1990.
70. Seifert V, Loffler BM, Zimmermann M, Roux S, Stolke D: Endothelin concentrations in patients with aneurysmal subarachnoid hemorrhage: Correlation with cerebral vasospasm, delayed ischemic neurological deficits, and volume of hematoma. J Neurosurg 82:55-62, 1995.
71. Shigeno T, Clozel M, Sakai S, Saito A, Goto K: The effect of bosentan, a new potent endothelin receptor antagonist, on the pathogenesis of cerebral vasospasm. Neurosurgery 37:86-91, 1995.
72. Shigeno T, Mima T, Takakura K, Yanagisawa M, Saito A, Goto K, Masaki T: Endothelin-1 acts in cerebral arteries from the adventitial but not from the luminal side. J Cardiovasc Pharmacol 13[Suppl 5]:5174-5176, 1989.
73. Shigeno T, Mima T, Yanagisawa M, Saito A, Fujimori A, Shiba R, Goto K, Kimura S, Yamashita K, Yamasaki Y, Masaki T, Takakura K: Possible role of endothelin in pathogenesis of cerebral vasospasm. J Cardiovasc Pharmacol 17[Suppl 7]:S480-S483, 1991.
74. Shinyama H, Uchida T, Kido H, Hayashi K, Watanabe M, Matsumura Y, Ikegawa R, Takaoka M, Morimoto S: Phosphoramidon inhibits the conversion of intracisternally administered big endothelin-1 to endothelin-1. Biochem Biophys Res Commun 178:24-30, 1991.
75. Shirakami G, Magaribuchi T, Shingu K, Kim S, Saito Y, Nakao K, Mori K: Changes of endothelin concentration in cerebrospinal fluid and plasma of patients with aneurysmal subarachnoid hemorrhage. Acta Anaesthesiol Scand 38:457-461, 1994.
76. Sokolovsky M: Endothelins and sarafotoxins: Physiological regulation, receptor subtypes and transmembrane signaling. Pharmacol Ther 54:129-149, 1992.
77. Suzuki H, Sato S, Suzuki Y, Oka M, Tsuchiya I, Iino I, Yamanaka T, Ishihara N, Shimoda S: Endothelin immunoreactivity in cerebrospinal fluid of patients with subarachnoid hemorrhage. Ann Med 22:233-236, 1990.
78. Suzuki H, Sato SH, Suzuki Y, Takekoshi K, Ishihara N, Shimoda S: Increased endothelin concentration in CSF from patients with subarachnoid hemorrhage. Acta Neural Scand 81:553-554, 1990.
79. Suzuki R, Masaoka H, Hirata Y, Marumo F, Isotani E, Hirakawa K: The role of endothelin-1 in the origin of cerebral vasospasm in patients with aneurysmal subarachnoid hemorrhage. J Neurosurg 77:96-100, 1992.
80. Umemura K, Ishiye M, Kosuge K, Nakashima M: Effect of combination of a tissue-type plasminogen activator and an endothelin receptor antagonist, FR139317, in the rat cerebral infarction model. Eur J Pharmacol 275:17-21, 1995.
81. Vane JR, Anggard EE, Botting RM: Regular functions of the vascular endothelium. N Engl J Med 323:27-36, 1990.
82. Wanebo JE, Louis HG, Arthur AS, Zhou J, Kassell NF, Lee KS, Helm GA: Systemic administration of an endothelin-A receptor antagonist, TBC 11251, attenuates cerebral vasospasm in a rabbit model of subarachnoid hemorrhage. Neurosurg Focus 3:Article 6, 1997.
83. Watanabe J, Asano T, Shimizu T, Seyami Y, Takakura K: Participation of lipoxygenase products from arachidonic acid in the pathogenesis of cerebral vasospasm. J Neurochem 50:1145-1150, 1988.
84. Weber C, Schmitt R, Birnboeck H, Hopfgartner G, van Marie SP, Peeters PAM, Jonkman JHG, Jones C: Pharmacokinetics and pharmacodynamics of the endothelin-receptor antagonist bosentan in healthy human subjects. Clin Pharmacol Ther 60:124-137, 1996.
85. Willette RN, Zhang H, Mitchell MP, Sauermelch CF, Ohlstein EH, Sulpizio AC: Nonpeptide endothelin antagonist: Cerebrovascular characterization and effects on delayed cerebral vasospasm. Stroke 25:2450-2456, 1994.
86. Wu C, Chan MF, Stavros F, Raju B, Okun I, Mong S, Keller KM, Brock T, Kogan TP, Dixon RAF: Discovery of TBC 11251, a potent, long acting, orally active endothelin receptor-A selective antagonist. J Med Chem 40:1690-1697, 1997.
87. Yamaura I, Tani E, Maeda Y, Minami N, Shindo H: Endothelin-1 of canine basilar artery in vasospasm. J Neurosurg 76:99-105, 1992.
88. Yanagisawa M, Kurihara H, Kimura S, Tomobe Y, Kobayashi M, Mitsui Y, Yazaki Y, Goto K, Masaki T: A novel potent vasoconstrictor peptide produced by vascular endothelial cells. Nature 332:411-115, 1988.
89. Yokokawa K, Kolmo M, Yasumari K, Murakawa K, Takeda T: Endothelin-3 regulates endothelin-1 production in human endothelial cells. Biochem Biophys Res Commun 188:286-291, 1992.
90. Yoshimoto S, Ishizaki Y, Kurihara H, Sasaki T, Yoshizumi M, Yanagisawa M, Yazaki Y, Masaki T, Takakura K, Muroto S: Cerebral microvessel endothelium is producing endothelin. Brain Res 508:283-285, 1990.
91. Zimmerman M, Seifert V, Loffler BM, Roux S, Stolke D: The role of big endothelin, endothelin-1 and endothelin-3 in the development of cerebral vasospasm and ischemic neurologic deficits after aneurysmal subarachnoid hemorrhage. Zentrabl Neurochir 45[Suppl]:82, 1994 (abstr).
92. Zimmerman M, Seifert V, Loffler BM, Stolke D, Stenzel W: Prevention of cerebral vasospasm after experimental subarachnoid hemorrhage by Ro 47-0203, a newly developed orally active endothelin receptor antagonist. Neurosurgery 38:115-120, 1996.
93. B receptors in subarachnoid hemorrhage-induced cerebral vasospasm. Eur J Pharmacol 259:R1-R2, 1994.
94. Zuccarello M, Romano A, Passalacqua M, Rapoport RM: Decreased endothelium-dependent relaxation in subarachnoid hemorrhage-induced vasospasm: Role of ET-1. Am J Physiol 269:H1009-H1015, 1995.
95. Zuccarello M, Soattin GB, Lewis AI, Breu V, Hallak H, Rapoport RM: Prevention of subarachnoid hemorrhage-induced cerebral vasospasm by oral administration of endothelin receptor antagonists. J Neurosurg 84:503-507, 1996.