Abstract
Diseases of the cardiovascular system account for the majority of morbidity and mortality in Western countries. Most forms of cardiovascular disease are associated with impaired vascular function in the cerebral, coronary, renal or peripheral circulation. Enhanced intermittent and/or persistent vasoconstriction is one of the most important features of several forms of cardiovascular disease [1]. Indeed, hypertension is characterized by a persistent increase in vascular tone of resistance arteries. In coronary spasm, migraine and Raynaud’s phenomenon, focal spasms of larger arteries are responsible for the clinical symptoms. Enhanced coronary vasoconstriction also importantly determines the angina threshold in patients with atherosclerotic coronary artery disease. Similarly, in low-tension glaucoma, increased vascular tone has been accounted for vision field defects and loss of sight [2]. Cerebral vasospasm after subarachnoid hemorrhage is an important complication associated with high morbidity and mortality in patients [3].
Access this chapter
Tax calculation will be finalised at checkout
Purchases are for personal use only
Preview
Unable to display preview. Download preview PDF.
References
Löscher TF, Vanhoutte PM (1990) The endothelium: modulator of cardiovascular function. CRC Press, Boca Raton
Gasser P, Flammer J (1987) Influence of vasospasm on visual function. Doc Ophthalmol 66: 3–18
Kassell NF, Sasaki T, Colohan ART, Nazar GB (1985) Cerebral vasospasm following aneurysmal subarachnoid hemorrhage. Stroke 16: 562–572
Yanagisawa M, Kurihara H, Kimura S, Tomobe Y, Kobayashi M, Mitsui Y, Yazaki Y, Goto K, Masaki T (1988) A novel potent vasoconstrictor peptide produced by vascular endothelial cells. Nature 332: 411–415
Yanagisawa M, Masaki T (1989) Molecular biology and biochemistry of the endothelins. Trends Pharmacol Sci 10: 374–378
Yanagisawa M, Inoue A, Ishikawa T, Kasuya Y, Kimura S, Kumagaye S, Nakajima K, Watanabe TX, Sakakibara S, Goto K, Masaki T (1988) Primary structure, synthesis, and biological activity of rat endothelin, an endothelium-derived vasoconstrictor peptide. Proc Natl Acad Sci USA 85: 6964–6967
Wagner OF, Christ G, Wojta J, Vierhapper H, Parzer S, Nowotny PJ, Schneider B, Waldhäusl W, Binder BR (1992) Polar secretion of endothelin-i by cultured endothelial cells. J Biol Chem 267: 16066–16068
Kurihara T, Akimoto M, Kurokawa K, Ishiguro H, Niimi A, Maeda A, Sigemoto M, Yamashita K, Yokoyama I, Hirayama Yet al (1992) ET-3 sensitive reduction of tissue blood flow in rat liver. Life Sci 51: 6
Karne S, Jayawickreme CK, Lerner MR (1993) Cloning and characterization of an endothelin-3 specific receptor ( ETC receptor) from Xenopus laevis dermal melanophores. J Biol Chem 268: 19126–19133
Seo B, Oemar BS, Siebenmann R, von Segesser L, Löscher TF (1994) Both ETA and ETB receptors mediate contraction to endothelin-i in human blood vessels. Circulation 89: 1203–1208
Kiowski W, Löscher TF, Linder L, Buhler FR (1991) Endothelin-s-induced vasoconstriction in humans. Reversal by calcium channel blockade but not by nitrovasodilators or endothelium-derived relaxing factor. Circulation 83: 469–475
Löscher TF, Yang Z, Tschudi M, Von SL, Stulz P, Boulanger C, Siebenmann R, Turina M, Buhler FR (1990) Interaction between endothelin-i and endothelium-derived relaxing factor in human arteries and veins. Circ Res 66: 1088–1094
Löscher TF, Boulanger CM, Dohi Y, Yang ZH (1992) Endothelium-derived contracting factors. Hypertension 19: 117–13o
Löscher TF (1993) Do we need endothelin antagonists? Cardiovasc Res 27: 2089–2093
Zamora MR, O’Brien RF, Rutherford RB, Weil JV (1990) Serum endothelin-i concentrations and cold provocation in primary Raynaud’s phenomenon (see comments). Lancet 336: 1144–1147
Cavero PG, Miller WL, Heublein DM, Margulies KB, Burnett JJ (1990) Endothelin in experimental congestive heart failure in the anesthetized dog. Am J Physiol (Renal Fluid Electrolyte Physiol) 259: 28–32
Cernacek P, Stewart DJ (1989) Immunoreactive endothelin in human plasma: marked elevations in patients in cardiogenic shock. Biochem Biophys Res Commun 161: 562–567
Margulies KB, Hildebrand FJ, Lerman A, Perrella MA, Burnett JJ (1990) Increased endothelin in experimental heart failure. Circulation 82: 2226–2230
Noll G, Tschudi MR, Novosel D, Lüscher TF (1994) Activity of the L-arginine/nitric oxide pathway and endothelin-i in experimental heart failure. J Cardiovasc Pharm 23: 916–921
Rodeheffer RJ, Lerman A, Heublein DM, Burnett JJ (1992) Increased plasma concentrations of endothelin in congestive heart failure in humans (see comments). Mayo Clin Proc 67: 719–724
Stewart DJ, Cernacek P, Costello KB, Rouleau JL (1992) Elevated endothelin-i in heart failure and loss of normal response to postural change. Circulation 85: 510–517
Cody RJ, Haas GJ, Binkley PF, Capers Q, Kelley R (1992) Plasma endothelin correlates with the extent of pulmonary hypertension in patients with chronic congestive heart failure. Circulation 85: 504–509
Zeiher A (1994) Endothelin in patients with unstable angina. Lancet 334: 1405–1406
Stewart DJ, Kubac G, Costello KB, Cernacek P (1991) Increased plasma endothelin-i in the early hours of acute myocardial infarction. J Am Coll Cardiol 18: 38–43
Lüscher TF, Seo BG, Bühler FR (1993) Potential role of endothelin in hypertension: Controversy of endothelin in hypertension. Hypertension 21: 752–757
Vanhoutte PM (1993) Is endothelin involved in the pathogenesis of hypertension? Hypertension 21 747–751
Yokokawa K, Tahara H, Kohno M, Murakawa K, Yasunari K, Nakagawa K, Hamada T, Otani S, Yanagisawa M, Takeda T (1991) Hypertension associated with endothelin-secreting malignant hemangioendothelioma. Ann Intern Med 114: 213–215
Larivière R, Thibault G, Schiffrin EL (1993) Increased endothelin-i content in blood vessels of deoxycorticosterone acetate-salt hypertensive rats but not in spontaneously hypertensive rats. Hypertension 21: 294–300
Nishikibe M, Tsuchida S, Okada M, Fukuroda T, Shimamoto K, Yano M, Ishikawa K, lkemoto F (1993) Antihypertensive effect of a newly synthesized endothelin antagonist, BQ-123, in a genetic hypertensive model. Life Sci 52: 717–724
Goerre S, Wenk M, Bartsch P, Lüscher TF, Niroomand S, Hohernhaus H, Hoelz O, Reinhart WH (1995) Endothelin-1 in pulmonary hypertension associated with high altitude. Circulation 90: 359–364
Kaiser H, Flammer J, Wenk M, Lüscher TFI (1995) Abnormal response of endothelin-i plasma levels to changes in posture in patients with low tension glaucoma. Arch Ophtalmol (in press)
Roubert P, Cornet S, Plas P, Guilmard C, Pirotzky E, Chabrier PE, Braquet P (1993) Upregulation of renal endothelin receptors in glycerol-induced acute renal failure in the rat. J Cardiovasc Pharmacol 22: S303 - S305
Tomita K, Ujiie K, Nakanishi T, Tomura S, Matsuda O, Ando K, Shichiri M, Hirata Y, Marumo F (1989) Plasma endothelin levels in patients with acute renal failure (letter). N Engl J Med 321: 16
Warrens AN, Cassidy MJ, Takahashi K, Ghatei MA, Bloom SR (1990) Endothelin in renal failure. Nephrol Dial Transplant 5: 418–422
Nambi P, Pullen M, Contino LC, Brooks DP (1990) Upregulation of renal endothelin receptors in rats with cyclosporine A-induced nephrotoxicity. Eur J Pharmacol 187: 113–116
Gellai M, Jugus M, Fletcher T, De Wolf R, Nambi P (1994) Reversal of postischemic acute renal failure with a selective endothelin. A receptor antagonist in the rat. J Clin Invest 93: 900–906
Vemulapalli S, Chiu PJ, Chintala M, Bernardino V (1993) Attenuation of ischemic acute renal failure by phosphoramidon in rats. Pharmacology 47: 188–193
Mallamaci F, Parlongo S, Zoccali C (1993) Influence of cardiovascular damage and residual renal function on plasma endothelin in chronic renal failure. Nephron 63: 291–295
Heyman SN, Clark BA, Kaiser N, Epstein FH, Spokes K, Rosen S, Brezis M (1992) In-vivo and in-vitro studies on the effect of amphotericin B on endothelin release. J Antimicrob Chemother 29: 69–77
Heyman SN, Clark BA, Kaiser N, Spokes K, Rosen S, Brezis M, Epstein FH (1992) Radiocontrast agents induce endothelin release in vivo and in vitro. J Am Soc Nephrol 3: 58–65
Heyman SN, Clark BA, Cantley L, Spokes K, Rosen S, Brezis M, Epstein FH (1993) Effects of ioversol versus iothalamate on endothelin release and radiocontrast nephropathy. Invest Radiol 28: 313–318
Cantley LG, Spokes K, Clark B, McMahon EG, Carter J, Epstein FH (1993) Role of endothelin and prostaglandins in radiocontrast-induced renal artery constriction. Kidney Int 44: 1217–1223
Ohta K, Hirata Y, Shichiri M, Ichioka M, Kubota T, Marumo F (1991) Cisplatin-induced urinary endothelin excretion (letter). JAMA 265: 1391–1392
Ong AC, Jowett TP, Scoble JE, O’Shea JA, Varghese Z, Moorhead JF (1993) Effect of cyclosporin A on endothelin synthesis by cultured human renal cortical epithelial cells. Nephrol Dial Transplant 8 748–753
Bunchman TE, Brookshire CA (1991) Cyclosporine-induced synthesis of endothelin by cultured human endothelial cells. J Clin Invest 88: 310–314
Iwasaki S, Homma T, Kon V (1994) Site specific regulation in the kidney of endothelin and its receptor subtypes by cyclosporine. Kidney Int 45: 592–597
Copeland KR, Yatscoff RW (1992) Comparison of the effects of cyclosporine and its metabolites on the release of prostacyclin and endothelin from mesangial cells. Transplantation 53: 640–645
Moutabarrik A, Ishibashi M, Fukunaga M, Kameoka H, Kawaguchi N, Takano Y, Kokado Y, Son-oda T, Onishi S, Takahara S et al (1992) FK5o6-induced kidney tubular cell injury. Transplantation 54: 1041–1047
Tschudi M, Richard V, Bühler FR, Lüscher TF (1991) Importance of endothelium-derived nitric oxide in porcine coronary resistance arteries. Am J Physiol 260: H13 - H20
Furchgott RF, Zawadzki JV (1980) The obligatory role of endothelial cells in the relaxation of arterial smooth muscle by acetylcholine. Nature 288: 373–376
Palmer RM, Ferrige AG, Moncada S (1987) Nitric oxide release accounts for the biological activity of endothelium-derived relaxing factor. Nature 327: 524–526
Busse R, Fichtner H, Luckhoff A, Kohlhardt M (1988) Hyperpolarization and increased free calcium in acetylcholine-stimulated endothelial cells. Am J Physiol 255: H965 - H969
Palmer RM, Ashton DS, Moncada S (1988) Vascular endothelial cells synthesize nitric oxide from L-arginine. Nature 333: 664–666
Yang ZH, Von SL, Bauer E, Stulz P, Turina M, Lüscher TF (1991) Different activation of the endothelial L-arginine and cyclooxygenase pathway in the human internal mammary artery and saphenous vein. Circ Res 68: 52–60
Lüscher TF, Diederich D, Siebenmann R, Lehmann K, Stulz P, Von SL, Yang ZH, Turina M, Gradel E, Weber E et al. (1988) Difference between endothelium-dependent relaxation in arterial and in venous coronary bypass grafts. N Engl J Med 319: 462–467
Richard V, Tanner FC, Tschudi M, Lüscher TF (1990) Different activation of L-arginine pathway by bradykinin, serotonin, and clonidine in coronary arteries. Am J Physiol 260: H13 - H20
Boulanger C, Lüscher TF (1990) Release of endothelin from the porcine aorta. Inhibition of endothelium-derived nitric oxide. J Clin 85: 587–590
Arai H, Hori S, Aramori I, Ohkubo H, Nakanishi S (1990) Cloning and expression of a cDNA encoding an endothelin receptor. Nature 348: 730–732
Sakurai T, Yanagisawa M, Takuwa Y, Miyazaki H, Kimura S, Goto K, Masaki T (1990) Cloning of a cDNA encoding a non-isopeptide-selective subtype of the endothelin receptor. Nature 348: 732–735
Vane J (1990) Endothelins come home to roost (news; comment). Nature 348: 973–975
Goto K, Kasuya Y, Matsuki N, Takuwa Y, Kurihara H, Ishikawa T, Kimura S, Yanagisawa M, Masaki T (1989) Endothelin activates the dihydropyridine-sensitive, voltage-dependent Ca(2+) channel in vascular smooth muscle. Proc Natl Acad Sci USA 86: 3915–3918
Yang Z, Bauer E, Von SL, Stulz P, Turina M, Lüscher TF (1990) Different mobilization of calcium in endothelin-i-induced contractions in human arteries and veins: effects of calcium antagonists. J Cardiovasc Pharmacol 16: 654–660
Resink TJ, Scott-Burden T, Bühler FR (1988) Endothelin stimulates phospholipase C in cultured vascular smooth muscle cells. Biochem Biophys Res Commun 157: 1360–1368
Walinöfer A, Weir S, Ruegg U, Cauvin C (1989) The mechanism of action of endothelin-1 as compared with other agonists in vascular smooth muscle. J Cardiovasc Pharmacol 13 [Suppl 5]: S23 - S31
Miller VM, Komori K, Burnett JC Jr, Vanhoutte PM (1989) Differential sensitivity to endothelin in canine arteries and veins. Am J Physiol 257: H1127 - H1131
Tabuchi Y, Nakamaru M, Rakugi H, Nagano M, Ogihara T (1989) Endothelin enhances adrenergic vasoconstriction in perfused rat mesenteric arteries. Biochem Biophys Res Commun 159 1304–1308
Yang Z, Richard V, Von SL, Bauer E, Stulz P, Turins M, Löscher TF (1990) Threshold concentrations of endothelin-1 potentiate contractions to norepinephrine and serotonin in human arteries. A new mechanism of vasospasm? Circulation 82: 188–195
Cauvin C, Tejerina M, Hwang O, Kai-Yamamoto M, van Breemen C (1988) The effects of Ca2+ antagonists on isolated rat and rabbit mesenteric resistance vessels. What determines the sensitivity of agonist-activated vessels to Ca2+-antagonists? Ann N Y Acad Sci 522: 338–350
Wenzel RR, Noll G, Löscher TF (1994) Endothelin receptor antagonists inhibit endothelin in human skin microcirculation. Hypertension 23: 581–586
Garg UC, Hassid A (1989) Nitric oxide-generating vasodilators and 8-bromo-cyclic guanosine monophosphate inhibit mitogenesis and proliferation of cultured rat vascular smooth muscle cells. J Clin Invest 83: 1774–1777
Yang Z, Noll G, Löscher TF (1993) Calcium antagonists differently inhibit proliferation of human coronary smooth muscle cells in response to pulsatile stretch and platelet-derived growth factor. Circulation 88: 832–836
Ullrich A, Schlessinger J (1990) Signal transduction by receptors with tyrosine kinase activity. Cell 61: 203–212
Henry PD, Bentley KI (1981) Suppression of atherogenesis in cholesterol-fed rabbit treated with nifedipine. J Clin Invest 68: 1366–1369
Lichtlen PR, Hugenholtz P, Rafflenbeul W, Jost S, Deckers JW (1990) Retardation of angiographic progression of coronary artery disease by nifedipine. Lancet 335: 1109–1113
Blankenhorn DH, Azen SP, Kramsch DM, Mack WJ, Cashin-Hemphill L, Hodis HN, De Boer LW, Mahrer PR, Masteller MJ, Vailas LI (1993) Coronary angiographic changes with lovastatin therapy. The Monitored Atherosclerosis Regression Study (MARS). The MARS Research Group. Ann Intern Med 119: 969–976
Dumont JM (1993) Effect of cholesterol reduction by simvastatin on progression of coronary atherosclerosis: design, baseline characteristics, and progress of the Multicenter Anti-Atheroma Study (MAAS). Control Clin Trials 14: 209–228
Aramori I, Nirei H, Shoubo M, Sogabe K, Nakamura K, Kojo H, Notsu Y, Ono T, Nakanishi S (1993) Subtype selectivity of a novel endothelin antagonist, FR 139317, for the two endothelin receptors in transfected Chinese hamster ovary cells. Mol Pharmacol 43: 127–131
Breu V, Löffler BM, Clozel M (1993) In vitro characterization of Ro 46–2005, a novel synthetic non-peptide endothelin antagonist of ETA and ETB receptors. FEBS Lett 334: 210–214
Fujimoto M, Mihara S, Nakajima S, Ueda M, Nakamura M, Sakurai K (1992) A novel non-peptide endothelin antagonist isolated from bayberry, Myrica cerifera. FEBS Lett 305: 41–44
Fukuroda T, Nishikibe M, Ohta Y, Ihara M, Yano M, Ishikawa K, Fukami T, Ikemoto F (1992) Analysis of responses to endothelins in isolated porcine blood vessels by using a novel endothelin antagonist, BQ-153. Life Sci 50: 12
Fukuroda T, Nishikibe M, Ihara M, Yano M, Ishikawa K, Ikemoto F (1992) Effects of a novel endothelin antagonist, BO-153, on endothelin-induced vasoconstriction in porcine blood vessels. Jpn J Pharmacol 58: 232–240
Ihara M, Noguchi K, Saeki T, Fukuroda T, Tsuchida S, Kimura S, Fukami T, Ishikawa K, Nishikibe M, Yano M (1992) Biological profiles of highly potent novel endothelin antagonists selective for the ETA receptor Life Sci 50: 247–255
Ishikawa K, Fukami T, Nagase T, Fujita K, Hayama T, Niiyama K, Mase T, Ihara M, Yano M (1992) Cyclic pentapeptide endothelin antagonists with high ETA selectivity. Potency-and solubility-enhancing modifications. J Med Chem 35: 2139–2142
Krystek SJ, Bassolino DA, Bruccoleri RE, Hunt JT, Porubcan MA, Wandler CF, Andersen NH (1992) Solution conformation of a cyclic pentapeptide endothelin antagonist. Comparison of structures obtained from constrained dynamics and conformational search. FEBS Lett 299: 255–261
Reily MD, Thanabal V, Omecinsky DO, Dunbar JJ, Doherty AM, DePue PL (1992) The solution structure of a cyclic endothelin antagonist, BQ-123, based on 1H–1H and 13C–1H three bond coupling constants. FEBS Lett 300: 136–140
Satoh T, Barlow D (1992) Molecular modelling of the structures of endothelin antagonists. Identification of a possible structural determinant for ET-A receptor binding. FEBS Lett 310: 83–87
Warner TD, Allcock GH, Corder R, Vane JR (1993) Use of the endothelin antagonists BQ-123 and PD 142 893 to reveal three endothelin receptors mediating smooth muscle contraction and the release of EDRF. Br J Pharmacol 110: 777–782
Sogabe K, Nirei H, Shoubo M, Nomoto A, Ao S, Notsu Y, Ono T (1993) Pharmacological profile of FR 139317, a novel, potent endothelin ETA receptor antagonist. J Pharmacol Exp Ther 264: 1040–1046
Tschudi MR, Löscher TF (1994) Characterization of contractile endothelin and angiotensin receptors in human resistance arteries: evidence for two endothelin and one angiotensin receptor. Biochem Biophys Res Commun 204: 685–690
Haynes WG, Strachan EF, Webb DJ (1994) ETB-receptors mediate vasoconstriction in vivo in man (abstract). Hypertension 24: 401
Haynes WG, Webb DJ (1994) Contribution of endogenous generation of endothelin-1 to basal vascular tone. Lancet 344: 852–854
Nayler WG (1992) Amlodipine. Springer, Berlin Heidelberg New York
Clozel M, Breu V, Burri K, Cassal JM, Fischli W, Gray GA, Hirth G, Loftier BM, Muller M, Neidhart W et al (1993) Pathophysiological role of endothelin revealed by the first orally active endothelin receptor antagonist. Nature 365: 759–761
Editor information
Editors and Affiliations
Rights and permissions
Copyright information
© 1995 Springer-Verlag Berlin Heidelberg
About this chapter
Cite this chapter
Wenzel, R.R., Lüscher, T.F. (1995). Endothelin Receptor Antagonists as New Tools to Inhibit Endothelin induced Vasoconstriction in Humans: Comparison with Calcium Channel Blockers. In: Lüscher, T.F. (eds) The Endothelium in Cardiovascular Disease. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-79803-0_11
Download citation
DOI: https://doi.org/10.1007/978-3-642-79803-0_11
Publisher Name: Springer, Berlin, Heidelberg
Print ISBN: 978-3-642-79805-4
Online ISBN: 978-3-642-79803-0
eBook Packages: Springer Book Archive