IUPHAR/BPS Guide to Pharmacology CITE
https://doi.org/10.2218/gtopdb/F21/2019.4

Endothelin receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database



Pedro D'Orléans-Juste1, Anthony P. Davenport2, Théophile Godfraind3, Janet J. Maguire2, Eliot H. Ohlstein4 and Robert R. Ruffolo5
  1. University of Sherbrooke, Canada
  2. University of Cambridge, UK
  3. Université Catholique de Louvain, Belgium
  4. Drexel University, USA
  5. Wyeth Pharmaceuticals, USA


Abstract

Endothelin receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Endothelin Receptors [24]) are activated by the endogenous 21 amino-acid peptides endothelins 1-3 (endothelin-1, endothelin-2 and endothelin-3).

Contents

This is a citation summary for Endothelin receptors in the Guide to Pharmacology database (GtoPdb). It exists purely as an adjunct to the database to facilitate the recognition of citations to and from the database by citation analyzers. Readers will almost certainly want to visit the relevant sections of the database which are given here under database links.

GtoPdb is an expert-driven guide to pharmacological targets and the substances that act on them. GtoPdb is a reference work which is most usefully represented as an on-line database. As in any publication this work should be appropriately cited, and the papers it cites should also be recognized. This document provides a citation for the relevant parts of the database, and also provides a reference list for the research cited by those parts.

Please note that the database version for the citations given in GtoPdb are to the most recent preceding version in which the family or its subfamilies and targets were substantially changed. The links below are to the current version. If you need to consult the cited version, rather than the most recent version, please contact the GtoPdb curators.

Database links

Endothelin receptors
http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=21
Introduction to Endothelin receptors
http://www.guidetopharmacology.org/GRAC/FamilyIntroductionForward?familyId=21
    Receptors
            ETA receptor
            http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=219
            ETB receptor
            http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=220

References

  1. Adachi M, Yang YY, Furuichi Y and Miyamoto C. (1991) Cloning and characterization of cDNA encoding human A-type endothelin receptor. Biochem. Biophys. Res. Commun. 180: 1265-72 [PMID:1719979]
  2. Adner M, Cardell LO, Sjöberg T, Ottosson A and Edvinsson L. (1996) Contractile endothelin-B (ETB) receptors in human small bronchi. Eur. Respir. J. 9: 351-5 [PMID:8777976]
  3. Arai H, Hori S, Aramori I, Ohkubo H and Nakanishi S. (1990) Cloning and expression of a cDNA encoding an endothelin receptor. Nature 348: 730-2 [PMID:2175396]
  4. Arai H, Nakao K, Takaya K, Hosoda K, Ogawa Y, Nakanishi S and Imura H. (1993) The human endothelin-B receptor gene. Structural organization and chromosomal assignment. J. Biol. Chem. 268: 3463-70 [PMID:8429023]
  5. Aramori I and Nakanishi S. (1992) Coupling of two endothelin receptor subtypes to differing signal transduction in transfected Chinese hamster ovary cells. J. Biol. Chem. 267: 12468-74 [PMID:1319997]
  6. Aramori I, Nirei H, Shoubo M, Sogabe K, Nakamura K, Kojo H, Notsu Y, Ono T and Nakanishi S. (1993) Subtype selectivity of a novel endothelin antagonist, FR139317, for the two endothelin receptors in transfected Chinese hamster ovary cells. Mol. Pharmacol. 43: 127-31 [PMID:8429819]
  7. Bacon CR and Davenport AP. (1996) Endothelin receptors in human coronary artery and aorta. Br. J. Pharmacol. 117: 986-92 [PMID:8851522]
  8. Balwierczak JL, Bruseo CW, DelGrande D, Jeng AY, Savage P and Shetty SS. (1995) Characterization of a potent and selective endothelin-B receptor antagonist, IRL 2500. J. Cardiovasc. Pharmacol. 26 Suppl 3: S393-6 [PMID:8587424]
  9. Battistini B, Berthiaume N, Kelland NF, Webb DJ and Kohan DE. (2006) Profile of past and current clinical trials involving endothelin receptor antagonists: the novel "-sentan" class of drug. Exp Biol Med (Maywood) 231: 653-695 [PMID:16740981]
  10. Battistini B and Dussault P. (1998) Biosynthesis, distribution and metabolism of endothelins in the pulmonary system. Pulm Pharmacol Ther 11: 79-88 [PMID:9918740]
  11. Baynash AG, Hosoda K, Giaid A, Richardson JA, Emoto N, Hammer RE and Yanagisawa M. (1994) Interaction of endothelin-3 with endothelin-B receptor is essential for development of epidermal melanocytes and enteric neurons. Cell 79: 1277-85 [PMID:8001160]
  12. Bolli MH, Boss C, Binkert C, Buchmann S, Bur D, Hess P, Iglarz M, Meyer S, Rein J and Rey M et al.. (2012) The discovery of N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propylsulfamide (Macitentan), an orally active, potent dual endothelin receptor antagonist. J. Med. Chem. 55: 7849-61 [PMID:22862294]
  13. Bolli MH, Marfurt J, Grisostomi C, Boss C, Binkert C, Hess P, Treiber A, Thorin E, Morrison K and Buchmann S et al.. (2004) Novel benzo[1,4]diazepin-2-one derivatives as endothelin receptor antagonists. J. Med. Chem. 47: 2776-95 [PMID:15139756]
  14. Breu V, Clozel M, Burri K, Hirth G, Neidhart W and Ramuz H. (1996) In vitro characterisation of Ro 46-8443, the first non-peptide antagonist selective for the endothelin ETB receptor. FEBS Lett. 383: 37-41 [PMID:8612786]
  15. Breu and V. et al.. (2003) Heterocyclic sulfonamides. Patent number: US6521631.
  16. Cai Y, Yamada T, Xin X, Agui T and Matsumoto K. (1995) Mapping of the genes for rat endothelin receptor type A (ETAR) and type B (ETBR) to chromosomes 19 and 15 respectively. Anim. Genet. 26: 39-41 [PMID:7702211]
  17. Cheng HF, Su YM, Yeh JR and Chang KJ. (1993) Alternative transcript of the nonselective-type endothelin receptor from rat brain. Mol. Pharmacol. 44: 533-8 [PMID:8371713]
  18. Clouthier DE, Hosoda K, Richardson JA, Williams SC, Yanagisawa H, Kuwaki T, Kumada M, Hammer RE and Yanagisawa M. (1998) Cranial and cardiac neural crest defects in endothelin-A receptor-deficient mice. Development 125: 813-24 [PMID:9449664]
  19. Clozel M, Breu V, Gray GA, Kalina B, Löffler BM, Burri K, Cassal JM, Hirth G, Müller M and Neidhart W et al.. (1994) Pharmacological characterization of bosentan, a new potent orally active nonpeptide endothelin receptor antagonist. J. Pharmacol. Exp. Ther. 270: 228-35 [PMID:8035319]
  20. Clozel M, Ramuz H, Clozel JP, Breu V, Hess P, Loffler BM, Coassolo P and Roux S. (1999) Pharmacology of tezosentan, new endothelin receptor antagonist designed for parenteral use. J. Pharmacol. Exp. Ther. 290: 840-846 [PMID:10411600]
  21. Cyr C, Huebner K, Druck T and Kris R. (1991) Cloning and chromosomal localization of a human endothelin ETA receptor. Biochem. Biophys. Res. Commun. 181: 184-90 [PMID:1659806]
  22. Dasgupta F, Mukherjee AK and Gangadhar N. (2002) Endothelin receptor antagonists--an overview. Curr. Med. Chem. 9: 549-75 [PMID:11945124]
  23. Davenport AP. (1997) Distribution of endothelin receptors. In Endothelins in Biology and Medicine Edited by Mille R, Pelton JT, Huggins J: CRC Press.: 45-68 [ISBN: 0849369754]
  24. Davenport AP. (2002) International Union of Pharmacology. XXIX. Update on endothelin receptor nomenclature. Pharmacol. Rev. 54: 219-26 [PMID:12037137]
  25. Davenport AP and Battistini B. (2002) Classification of endothelin receptors and antagonists in clinical development. Clin. Sci. 103 Suppl 48: 1S-3S [PMID:12193042]
  26. Davenport AP, Kuc RE, Ashby MJ, Patt WC and Doherty AM. (1998) Characterization of [125I]-PD164333, an ETA selective non-peptide radiolabelled antagonist, in normal and diseased human tissues. Br. J. Pharmacol. 123: 223-30 [PMID:9489609]
  27. Davenport AP, Kuc RE, Fitzgerald F, Maguire JJ, Berryman K and Doherty AM. (1994) [125I]-PD151242: a selective radioligand for human ETA receptors. Br. J. Pharmacol. 111: 4-6 [PMID:8012722]
  28. Davenport AP and Maguire JJ. (2002) Of mice and men: advances in endothelin research and first antagonist gains FDA approval. Trends Pharmacol. Sci. 23: 155-7 [PMID:11931980]
  29. Davenport AP and Maguire JJ. (2006) Endothelin. Handb Exp Pharmacol 295-329 [PMID:16999223]
  30. Davenport AP, O'Reilly G and Kuc RE. (1995) Endothelin ETA and ETB mRNA and receptors expressed by smooth muscle in the human vasculature: majority of the ETA sub-type. Br. J. Pharmacol. 114: 1110-6 [PMID:7620699]
  31. Davenport AP and Russell FD. (2001) Endothelin converting enzymes and endothelin receptor localisation in human tissues. Handb. Exp. Pharmacol. 152: 209-237
  32. de Nucci G, Thomas R, D'Orleans-Juste P, Antunes E, Walder C, Warner TD and Vane JR. (1988) 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. Proc. Natl. Acad. Sci. U.S.A. 85: 9797-800 [PMID:3059352]
  33. De Oliveira AM, Viswanathan M, Capsoni S, Heemskerk FM, Correa FM and Saavedra JM. (1995) Characterization of endothelinA receptors in cerebral and peripheral arteries of the rat. Peptides 16: 139-44 [PMID:7716066]
  34. Dhein S, Giessler C, Wangemann T, Silber RE, Zerkowski HR and Brodde OE. (2000) Differential pattern of endothelin-1-induced inotropic effects in right atria and left ventricles of the human heart. J. Cardiovasc. Pharmacol. 36: 564-9 [PMID:11065215]
  35. Doherty AM, Patt WC, Edmunds JJ, Berryman KA, Reisdorph BR, Plummer MS, Shahripour A, Lee C, Cheng XM and Walker DM et al.. (1995) Discovery of a novel series of orally active non-peptide endothelin-A (ETA) receptor-selective antagonists. J. Med. Chem. 38: 1259-63 [PMID:7731010]
  36. Douglas SA, Beck Jr GR, Elliott JD and Ohlstein EH. (1995) Pharmacologic evidence for the presence of three functional endothelin receptor subtypes in rabbit saphenous vein. J. Cardiovasc. Pharmacol. 26 Suppl 3: S163-8 [PMID:8587352]
  37. Douglas SA and Ohlstein EH. (1997) Signal transduction mechanisms mediating the vascular actions of endothelin. J. Vasc. Res. 34: 152-64 [PMID:9226297]
  38. Elliott JD, Lago MA, Cousins RD, Gao A, Leber JD, Erhard KF, Nambi P, Elshourbagy NA, Kumar C and Lee JA et al.. (1994) 1,3-Diarylindan-2-carboxylic acids, potent and selective non-peptide endothelin receptor antagonists. J. Med. Chem. 37: 1553-7 [PMID:8201588]
  39. Elliott JD, Ohlstein EH, Peishoff CE, Ellens HM and Lago MA. (1998) Endothelin receptor antagonists. Pharm Biotechnol 11: 113-29 [PMID:9760678]
  40. Elshourbagy NA, Adamou JE, Gagnon AW, Wu HL, Pullen M and Nambi P. (1996) Molecular characterization of a novel human endothelin receptor splice variant. J. Biol. Chem. 271: 25300-25307 [PMID:8810293]
  41. Elshourbagy NA, Korman DR, Wu HL, Sylvester DR, Lee JA, Nuthalaganti P, Bergsma DJ, Kumar CS and Nambi P. (1993) Molecular characterization and regulation of the human endothelin receptors. J. Biol. Chem. 268: 3873-9 [PMID:8440682]
  42. Fukuroda T, Fujikawa T, Ozaki S, Ishikawa K, Yano M and Nishikibe M. (1994) Clearance of circulating endothelin-1 by ETB receptors in rats. Biochem. Biophys. Res. Commun. 199: 1461-5 [PMID:8147891]
  43. Gardiner SM, Compton AM and Bennett T. (1989) Regional hemodynamic effects of endothelin-1 in conscious, unrestrained, Wistar rats. J. Cardiovasc. Pharmacol. 13 Suppl 5: S202-4 [PMID:2473311]
  44. Gardiner SM, Compton AM, Kemp PA and Bennett T. (1990) Regional and cardiac haemodynamic effects of NG-nitro-L-arginine methyl ester in conscious, Long Evans rats. Br. J. Pharmacol. 101: 625-31 [PMID:2076481]
  45. Gellai M, De Wolf R, Fletcher T and Nambi P. (1997) Contribution of endogenous endothelin-1 to the maintenance of vascular tone: role of nitric oxide. Pharmacology 55: 299-308 [PMID:9413859]
  46. Griswold DE, Douglas SA, Martin LD, Davis TG, Davis L, Ao Z, Luttmann MA, Pullen M, Nambi P and Hay DW et al.. (1999) Endothelin B receptor modulates inflammatory pain and cutaneous inflammation. Mol. Pharmacol. 56: 807-12 [PMID:10496965]
  47. Harland SP, Kuc RE, Pickard JD and Davenport AP. (1995) Characterization of endothelin receptors in human brain cortex, gliomas, and meningiomas. J. Cardiovasc. Pharmacol. 26 Suppl 3: S408-11 [PMID:8587429]
  48. Hatae N, Aksentijevich N, Zemkova HW, Kretschmannova K, Tomic M and Stojilkovic SS. (2007) Cloning and functional identification of novel endothelin receptor type A isoforms in pituitary. Mol. Endocrinol. 21: 1192-204 [PMID:17312275]
  49. Haynes WG and Webb DJ. (1994) Contribution of endogenous generation of endothelin-1 to basal vascular tone. Lancet 344: 852-4 [PMID:7916401]
  50. Horstmeyer A, Cramer H, Sauer T, Müller-Esterl W and Schroeder C. (1996) Palmitoylation of endothelin receptor A. Differential modulation of signal transduction activity by post-translational modification. J. Biol. Chem. 271: 20811-9 [PMID:8702836]
  51. Hoshino T, Yamauchi R, Kikkawa K, Yabana H and Murata S. (1998) Pharmacological profile of T-0201, a highly potent and orally active endothelin receptor antagonist. J. Pharmacol. Exp. Ther. 286: 643-9 [PMID:9694915]
  52. Hosoda K, Hammer RE, Richardson JA, Baynash AG, Cheung JC, Giaid A and Yanagisawa M. (1994) Targeted and natural (piebald-lethal) mutations of endothelin-B receptor gene produce megacolon associated with spotted coat color in mice. Cell 79: 1267-76 [PMID:8001159]
  53. Hosoda K, Nakao K, Hiroshi-Arai, Suga S, Ogawa Y, Mukoyama M, Shirakami G, Saito Y, Nakanishi S and Imura H. (1991) Cloning and expression of human endothelin-1 receptor cDNA. FEBS Lett. 287: 23-6 [PMID:1652463]
  54. Iglarz M, Binkert C, Morrison K, Fischli W, Gatfield J, Treiber A, Weller T, Bolli MH, Boss C and Buchmann S et al.. (2008) Pharmacology of macitentan, an orally active tissue-targeting dual endothelin receptor antagonist. J. Pharmacol. Exp. Ther. 327: 736-45 [PMID:18780830]
  55. Ihara M, Noguchi K, Saeki T, Fukuroda T, Tsuchida S, Kimura S, Fukami T, Ishikawa K, Nishikibe M and Yano M. (1992) Biological profiles of highly potent novel endothelin antagonists selective for the ETA receptor. Life Sci. 50: 247-55 [PMID:1310132]
  56. Ihara M, Saeki T, Fukuroda T, Kimura S, Ozaki S, Patel AC and Yano MA. (1992) Novel radioligand [125I]BQ-3020 selective for endothelin (ETB) receptors. Life Sci. 51: PL47-PL52 [PMID:1321937]
  57. Ihara M, Yamanaka R, Ohwaki K, Ozaki S, Fukami T, Ishikawa K, Towers P and Yano M. (1995) [3H]BQ-123, a highly specific and reversible radioligand for the endothelin ETA receptor subtype. Eur. J. Pharmacol. 274: 1-6 [PMID:7768260]
  58. Inoue A, Yanagisawa M, Kimura S, Kasuya Y, Miyauchi T, Goto K and Masaki T. (1989) The human endothelin family: three structurally and pharmacologically distinct isopeptides predicted by three separate genes. Proc. Natl. Acad. Sci. U.S.A. 86: 2863-7 [PMID:2649896]
  59. Ishikawa K, Ihara M, Noguchi K, Mase T, Mino N, Saeki T, Fukuroda T, Fukami T, Ozaki S and Nagase T et al.. (1994) Biochemical and pharmacological profile of a potent and selective endothelin B-receptor antagonist, BQ-788. Proc. Natl. Acad. Sci. U.S.A. 91: 4892-6 [PMID:8197152]
  60. Jae HS, Winn M, von Geldern TW, Sorensen BK, Chiou WJ, Nguyen B, Marsh KC and Opgenorth TJ. (2001) Pyrrolidine-3-carboxylic acids as endothelin antagonists. 5. Highly selective, potent, and orally active ET(A) antagonists. J. Med. Chem. 44: 3978-84 [PMID:11689084]
  61. Johnström P, Harris NG, Fryer TD, Barret O, Clark JC, Pickard JD and Davenport AP. (2002) (18)F-Endothelin-1, a positron emission tomography (PET) radioligand for the endothelin receptor system: radiosynthesis and in vivo imaging using microPET. Clin. Sci. 103 Suppl 48: 4S-8S [PMID:12193043]
  62. Karet FE, Kuc RE and Davenport AP. (1993) Novel ligands BQ123 and BQ3020 characterize endothelin receptor subtypes ETA and ETB in human kidney. Kidney Int. 44: 36-42 [PMID:8355464]
  63. Karne S Jayawickreme CK and Lerner MR. (1993) Cloning and characteriztion of an endothelin-3 specific receptor (ETC receptor) fromXenopus laevisdermal melanophores. J. Biol. Chem. 268: 19126-19133 [PMID:8360195]
  64. Kilpatrick SJ, Roberts JM, Lykins DL and Taylor RN. (1993) Characterization and ontogeny of endothelin receptors in human placenta. Am. J. Physiol. 264: E367-72 [PMID:8460684]
  65. Kondo S, Morita T and Tashima Y. (1994) Endothelin receptor density in human hypertrophic and non-hypertrophic prostate tissue. Tohoku J. Exp. Med. 172: 381-4 [PMID:7524189]
  66. Kuc RE, Karet FE and Davenport AP. (1995) Characterization of peptide and nonpeptide antagonists in human kidney. J. Cardiovasc. Pharmacol. 26 Suppl 3: S373-5 [PMID:8587419]
  67. Kusumoto K, Kubo K, Kandori H, Kitayoshi T, Sato S, Wakimasu M, Watanabe T and Fujino M. (1994) Effects of a new endothelin antagonist, TAK-044, on post-ischemic acute renal failure in rats. Life Sci. 55: 301-10 [PMID:8028448]
  68. Lin HY, Kaji EH, Winkel GK, Ives HE and Lodish HF. (1991) Cloning and functional expression of a vascular smooth muscle endothelin 1 receptor. Proc. Natl. Acad. Sci. U.S.A. 88: 3185-9 [PMID:1849646]
  69. MacCarthy PA, Grocott-Mason R, Prendergast BD and Shah AM. (2000) Contrasting inotropic effects of endogenous endothelin in the normal and failing human heart: studies with an intracoronary ET(A) receptor antagonist. Circulation 101: 142-7 [PMID:10637200]
  70. Maguire JJ and Davenport AP. (1995) ETA receptor-mediated constrictor responses to endothelin peptides in human blood vessels in vitro. Br. J. Pharmacol. 115: 191-7 [PMID:7647976]
  71. Maguire JJ, Kuc RE and Davenport AP. (1997) Affinity and selectivity of PD156707, a novel nonpeptide endothelin antagonist, for human ET(A) and ET(B) receptors. J. Pharmacol. Exp. Ther. 280: 1102-8 [PMID:9023329]
  72. Maguire JJ, Kuc RE, Doherty AM and Davenport AP. (1995) Potency of PD155080, an orally active ETA receptor antagonist, determined for human endothelin receptors. J. Cardiovasc. Pharmacol. 26 Suppl 3: S362-4 [PMID:8587415]
  73. Mizuguchi T, Nishiyama M, Moroi K, Tanaka H, Saito T, Masuda Y, Masaki T, de Wit D, Yanagisawa M and Kimura S. (1997) Analysis of two pharmacologically predicted endothelin B receptor subtypes by using the endothelin B receptor gene knockout mouse. Br. J. Pharmacol. 120: 1427-30 [PMID:9113361]
  74. Molenaar P, Kuc RE and Davenport AP. (1992) Characterization of two new ETB selective radioligands, [125I]-BQ3020 and [125I]-[Ala1,3,11,15]ET-1 in human heart. Br. J. Pharmacol. 107: 637-9 [PMID:1472961]
  75. Moravec CS, Reynolds EE, Stewart RW and Bond M. (1989) Endothelin is a positive inotropic agent in human and rat heart in vitro. Biochem. Biophys. Res. Commun. 159: 14-8 [PMID:2647079]
  76. Morphy R and Rankovic Z. (2005) Designed multiple ligands. An emerging drug discovery paradigm. J. Med. Chem. 48: 6523-43 [PMID:16220969]
  77. Morris CD, Rose A, Curwen J, Hughes AM, Wilson DJ and Webb DJ. (2005) Specific inhibition of the endothelin A receptor with ZD4054: clinical and pre-clinical evidence. Br. J. Cancer 92: 2148-52 [PMID:15956965]
  78. Murugesan N, Gu Z, Spergel S, Young M, Chen P, Mathur A, Leith L, Hermsmeier M, Liu EC and Zhang R et al.. (2003) Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective antagonist. J. Med. Chem. 46: 125-37 [PMID:12502366]
  79. Nagase T, Aoki T, Oka T, Fukuchi Y and Ouchi Y. (1997) ET-1-induced bronchoconstriction is mediated via ETB receptor in mice. J. Appl. Physiol. 83: 46-51 [PMID:9216943]
  80. Nakamuta M, Takayanagi R, Sakai Y, Sakamoto S, Hagiwara H, Mizuno T, Saito Y, Hirose S, Yamamoto M and Nawata H. (1991) Cloning and sequence analysis of a cDNA encoding human non-selective type of endothelin receptor. Biochem. Biophys. Res. Commun. 177: 34-39 [PMID:1710450]
  81. Nambi P, Pullen M and Spielman W. (1994) Species differences in the binding characteristics of [125I]IRL-1620, a potent agonist specific for endothelin-B receptors. J. Pharmacol. Exp. Ther. 268: 202-7 [PMID:8301559]
  82. O'Donnell SR and Kay CS. (1995) Effects of endothelin receptor selective antagonists, BQ-123 and BQ-788, on IRL 1620 and endothelin-1 responses of airway and vascular preparations from rats. Pulm Pharmacol 8: 11-9 [PMID:8535094]
  83. Ogawa Y, Nakao K, Arai H, Nakagawa O, Hosoda K, Suga S, Nakanishi S and Imura H. (1991) Molecular cloning of a non-isopeptide-selective human endothelin receptor. Biochem. Biophys. Res. Commun. 178: 248-55 [PMID:1648908]
  84. Ohlstein EH, Beck Jr GR, Douglas SA, Nambi P, Lago MA, Gleason JG, Ruffolo Jr RR, Feuerstein G and Elliott JD. (1994) Nonpeptide endothelin receptor antagonists. II. Pharmacological characterization of SB 209670. J. Pharmacol. Exp. Ther. 271: 762-8 [PMID:7965794]
  85. Ohlstein EH, Nambi P, Hay DW, Gellai M, Brooks DP, Luengo J, Xiang JN and Elliott JD. (1998) Nonpeptide endothelin receptor antagonists. XI. Pharmacological characterization of SB 234551, a high-affinity and selective nonpeptide ETA receptor antagonist. J. Pharmacol. Exp. Ther. 286: 650-6 [PMID:9694916]
  86. Ohlstein EH, Nambi P, Lago A, Hay DW, Beck G, Fong KL, Eddy EP, Smith P, Ellens H and Elliott JD. (1996) Nonpeptide endothelin receptor antagonists. VI: Pharmacological characterization of SB 217242, a potent and highly bioavailable endothelin receptor antagonist. J. Pharmacol. Exp. Ther. 276: 609-15 [PMID:8632328]
  87. Okazaki Y, Furuno M, Kasukawa T, Adachi J, Bono H, Kondo S, Nikaido I, Osato N, Saito R and Suzuki H et al.. (2002) Analysis of the mouse transcriptome based on functional annotation of 60,770 full-length cDNAs. Nature 420: 563-73 [PMID:12466851]
  88. Opgenorth TJ, Adler AL, Calzadilla SV, Chiou WJ, Dayton BD, Dixon DB, Gehrke LJ, Hernandez L, Magnuson SR and Marsh KC et al.. (1996) Pharmacological characterization of A-127722: an orally active and highly potent ETA-selective receptor antagonist. J. Pharmacol. Exp. Ther. 276: 473-81 [PMID:8632312]
  89. Panek RL, Major TC, Hingorani GP, Doherty AM, Taylor DG and Rapundalo ST. (1992) Endothelin and structurally related analogs distinguish between endothelin receptor subtypes. Biochem. Biophys. Res. Commun. 183: 566-71 [PMID:1312833]
  90. Peter MG and Davenport AP. (1995) Selectivity of [125I]-PD151242 for human, rat and porcine endothelin ETA receptors in the heart. Br. J. Pharmacol. 114: 297-302 [PMID:7881728]
  91. Pierre LN and Davenport AP. (1999) Blockade and reversal of endothelin-induced constriction in pial arteries from human brain. Stroke 30: 638-43 [PMID:10066864]
  92. Pollock DM and Highsmith RF. (1998) Endothelin receptors and signalling mechanisms. Springer: 1-224 [ISBN: 3540559701]
  93. Puffenberger EG, Hosoda K, Washington SS, Nakao K, deWit D, Yanagisawa M and Chakravart A. (1994) A missense mutation of the endothelin-B receptor gene in multigenic Hirschsprung's disease. Cell 79: 1257-66 [PMID:8001158]
  94. Reynolds EE, Hwang O, Flynn MA, Welch KM, Cody WL, Steinbaugh B, He JX, Chung FZ and Doherty AM. (1995) Pharmacological differences between rat and human endothelin B receptors. Biochem. Biophys. Res. Commun. 209: 506-12 [PMID:7733918]
  95. Riechers H, Albrecht HP, Amberg W, Baumann E, Bernard H, Böhm HJ, Klinge D, Kling A, Müller S and Raschack M et al.. (1996) Discovery and optimization of a novel class of orally active nonpeptidic endothelin-A receptor antagonists. J. Med. Chem. 39: 2123-8 [PMID:8667356]
  96. Russell A and Watts S. (2000) Vascular reactivity of isolated thoracic aorta of the C57BL/6J mouse. J. Pharmacol. Exp. Ther. 294: 598-604 [PMID:10900237]
  97. Russell FD and Davenport AP. (1996) Characterization of the binding of endothelin ETB selective ligands in human and rat heart. Br. J. Pharmacol. 119: 631-6 [PMID:8904635]
  98. Saeki T, Ihara M, Fukuroda T, Yamagiwa M and Yano M. (1991) [Ala1,3,11,15] endothelin-1 analogs with ETB agonistic activity. Biochem. Biophys. Res. Commun. 179: 286-292 [PMID:1652952]
  99. Saito Y, Mizuno T, Itakura M, Suzuki Y, Ito T, Hagiwara H and Hirose S. (1991) Primary structure of bovine endothelin ETB receptor and identification of signal peptidase and metal proteinase cleavage sites. J. Biol. Chem. 266: 23433-7 [PMID:1660473]
  100. Sakamoto A, Yanagisawa M, Sakurai T, Takuwa Y, Yanagisawa H and Masaki T. (1991) Cloning and functional expression of human cDNA for the ETB endothelin receptor. Biochem. Biophys. Res. Commun. 178: 656-63 [PMID:1713452]
  101. Sakurai T, Yanagisawa M, Takuwa Y, Miyazaki H, Kimura S, Goto K and Masaki T. (1990) Cloning of a cDNA encoding a non-isopeptide-selective subtype of the endothelin receptor. Nature 348: 732-5 [PMID:2175397]
  102. Schneider MP, Boesen EI and Pollock DM. (2007) Contrasting actions of endothelin ET(A) and ET(B) receptors in cardiovascular disease. Annu. Rev. Pharmacol. Toxicol. 47: 731-59 [PMID:17002597]
  103. Shihoya W, Izume T, Inoue A, Yamashita K, Kadji FMN, Hirata K, Aoki J, Nishizawa T and Nureki O. (2018) Crystal structures of human ETB receptor provide mechanistic insight into receptor activation and partial activation. Nat Commun 9: 4711 [PMID:30413709]
  104. Shihoya W, Nishizawa T, Yamashita K, Inoue A, Hirata K, Kadji FMN, Okuta A, Tani K, Aoki J and Fujiyoshi Y et al.. (2017) X-ray structures of endothelin ETB receptor bound to clinical antagonist bosentan and its analog. Nat. Struct. Mol. Biol. 24: 758-764 [PMID:28805809]
  105. Shyamala V, Moulthrop TH, Stratton Thomas J and Tekamp Olson P. (1994) Two distinct human endothelin B receptors generated by alternative splicing from a single gene. Cell. Mol. Biol. Res. 40: 285-296 [PMID:7866430]
  106. Simonson MS. (2001) Cell signalling by endothelin peptides. Handb. Exp. Pharm. 152: 115-140
  107. Stein PD, Hunt JT, Floyd DM, Moreland S, Dickinson KE, Mitchell C, Liu EC, Webb ML, Murugesan N and Dickey J et al.. (1994) The discovery of sulfonamide endothelin antagonists and the development of the orally active ETA antagonist 5-(dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulf onamide. J. Med. Chem. 37: 329-31 [PMID:8308857]
  108. Strachan FE, Spratt JC, Wilkinson IB, Johnston NR, Gray GA and Webb DJ. (1999) Systemic blockade of the endothelin-B receptor increases peripheral vascular resistance in healthy men. Hypertension 33: 581-5 [PMID:9931169]
  109. Takai M, Umemura I, Yamasaki K, Watakabe T, Fujitani Y, Oda K, Urade Y, Inui T, Yamamura T and Okada T. (1992) A potent and specific agonist, Suc-[Glu9,Ala11,15]-endothelin-1(8-21), IRL 1620, for the ETB receptor. Biochem. Biophys. Res. Commun. 184: 953-9 [PMID:1315540]
  110. Takigawa M, Sakurai T, Kasuya Y, Abe Y, Masaki T and Goto K. (1995) Molecular identification of guanine-nucleotide-binding regulatory proteins which couple to endothelin receptors. Eur. J. Biochem. 228: 102-8 [PMID:7882989]
  111. Tanaka H, Moroi K, Iwai J, Takahashi H, Ohnuma N, Hori S, Takimoto M, Nishiyama M, Masaki T and Yanagisawa M et al.. (1998) Novel mutations of the endothelin B receptor gene in patients with Hirschsprung's disease and their characterization. J. Biol. Chem. 273: 11378-83 [PMID:9556633]
  112. Tanaka T, Tsukuda E, Nozawa M, Nonaka H, Ohno T, Kase H, Yamada K and Matsuda Y. (1994) RES-701-1, a novel, potent, endothelin type B receptor-selective antagonist of microbial origin. Mol. Pharmacol. 45: 724-30 [PMID:8183252]
  113. Uhlig S, von Bethmann AN, Featherstone RL and Wendel A. (1995) Pharmacologic characterization of endothelin receptor responses in the isolated perfused rat lung. Am. J. Respir. Crit. Care Med. 152: 1449-60 [PMID:7582276]
  114. von Geldern TW, Tasker AS, Sorensen BK, Winn M, Szczepankiewicz BG, Dixon DB, Chiou WJ, Wang L, Wessale JL and Adler A et al.. (1999) Pyrrolidine-3-carboxylic acids as endothelin antagonists. 4. Side chain conformational restriction leads to ET(B) selectivity. J. Med. Chem. 42: 3668-78 [PMID:10479298]
  115. Warner TD, Allcock GH, Mickley EJ, Corder R and Vane JR. (1993) Comparative studies with the endothelin receptor antagonists BQ-123 and PD 142893 indicate at least three endothelin receptors. J. Cardiovasc. Pharmacol. 22 Suppl 8: S117-20 [PMID:7509920]
  116. Warner TD, de Nucci G and Vane JR. (1989) Rat endothelin is a vasodilator in the isolated perfused mesentery of the rat. Eur. J. Pharmacol. 159: 325-6 [PMID:2646137]
  117. Watakabe T, Urade Y, Takai M, Umemura I and Okada T. (1992) A reversible radioligand specific for the ETB receptor: [125I]Tyr13-Suc-[Glu9,Ala11,15]-endothelin-1(8- 21), [125I]IRL 1620. Biochem. Biophys. Res. Commun. 185: 867-73 [PMID:1320877]
  118. Watanabe T, Awane Y, Ikeda S, Fujiwara S, Kubo K, Kikuchi T, Kusumoto K, Wakimasu M and Fujino M. (1995) Pharmacology of a non-selective ETA and ETB receptor antagonist, TAK-044 and the inhibition of myocardial infarct size in rats. Br. J. Pharmacol. 114: 949-54 [PMID:7780649]
  119. Williams Jr DL, Jones KL, Pettibone DJ, Lis EV and Clineschmidt BV. (1991) Sarafotoxin S6c: an agonist which distinguishes between endothelin receptor subtypes. Biochem. Biophys. Res. Commun. 175: 556-61 [PMID:1850245]
  120. Williams Jr DL, Murphy KL, Nolan NA, O'Brien JA, Pettibone DJ, Kivlighn SD, Krause SM, Lis Jr EV, Zingaro GJ and Gabel RA et al.. (1995) Pharmacology of L-754,142, a highly potent, orally active, nonpeptidyl endothelin antagonist. J. Pharmacol. Exp. Ther. 275: 1518-26 [PMID:8531124]
  121. Williams RJ. (1988) Self-assembling surfaces. Nature 332: 393 [PMID:3352739]
  122. Winn M, von Geldern TW, Opgenorth TJ, Jae HS, Tasker AS, Boyd SA, Kester JA, Mantei RA, Bal R and Sorensen BK et al.. (1996) 2,4-Diarylpyrrolidine-3-carboxylic acids--potent ETA selective endothelin receptor antagonists. 1. Discovery of A-127722. J. Med. Chem. 39: 1039-48 [PMID:8676339]
  123. Wu C, Chan MF, Stavros F, Raju B, Okun I, Mong S, Keller KM, Brock T, Kogan TP and Dixon RA. (1997) Discovery of TBC11251, a potent, long acting, orally active endothelin receptor-A selective antagonist. J. Med. Chem. 40: 1690-7 [PMID:9171878]
  124. Wu C, Decker ER, Holland GW, Brown PM, Stavros FD, Brock TA and Dixon RA. (2001) Nonpeptide endothelin antagonists in clinical development. Drugs Today 37: 441-453 [PMID:12750762]
  125. Yamaji T, Fukuhara T and Kinoshita M. (1993) Increased capillary permeability to albumin in diabetic rat myocardium. Circ. Res. 72: 947-57 [PMID:8477528]
  126. Yanagisawa H, Hammer RE, Richardson JA, Williams SC, Clouthier DE and Yanagisawa M. (1998) Role of Endothelin-1/Endothelin-A receptor-mediated signaling pathway in the aortic arch patterning in mice. J. Clin. Invest. 102: 22-33 [PMID:9649553]
  127. Zhang YF, Jeffery S, Burchill SA, Berry PA, Kaski JC and Carter ND. (1998) Truncated human endothelin receptor A produced by alternative splicing and its expression in melanoma. Br. J. Cancer 78: 1141-6 [PMID:9820169]