More information on this family may be found on the IUPHAR-DB family and introduction pages.
Endothelin receptors (nomenclature as agreed by NC-IUPHAR Subcommittee on endothelin receptors, [3]) are activated by the endogenous 21 amino-acid peptides endothelin-1 (ET-1, ENSG00000078401), ET-2 (ENSG00000127129) and ET-3 (ENSG00000124205). Non-selective peptide (e.g. TAK 044, pA2 8.4) and non-peptide (e.g. bosentan, pA2 6.0–7.2; SB209670, pA2 9.4) antagonists can block both ETA and ETB receptors. Splice variants of the ETA receptor have been identified in rat pituitary cells; one of these, ETAR-C13, appeared to show loss of function with comparable plasma membrane expression [7].
Unless otherwise stated all data refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).
Receptors 
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Bagnato, A; Rosanò, L. (2008) The endothelin axis in cancer. Int. J. Biochem. Cell Biol., 40 (8): 1443-51. [PMID:18325824]
Davenport, A. P. (2002) International Union of Pharmacology. XXIX. Update on endothelin receptor nomenclature. . Pharmacol. Rev., 54: 219-226. [PMID:12037137]
Dhaun, N; Goddard, J; Kohan, DE; Pollock, DM; Schiffrin, EL; Webb, DJ. (2008) Role of endothelin-1 in clinical hypertension: 20 years on. Hypertension, 52 (3): 452-9. [PMID:18678788]
Dhaun, N; Pollock, DM; Goddard, J; Webb, DJ. (2007) Selective and mixed endothelin receptor antagonism in cardiovascular disease. Trends Pharmacol. Sci., 28 (11): 573-9. [PMID:17950470]
Dupuis, J; Hoeper, MM. (2008) Endothelin receptor antagonists in pulmonary arterial hypertension. Eur. Respir. J., 31 (2): 407-15. [PMID:18238950]
Kawanabe, Y; Nauli, SM. (2011) Endothelin. Cell. Mol. Life Sci., 68 (2): 195-203. [PMID:20848158]
Khodorova, A; Montmayeur, JP; Strichartz, G. (2009) Endothelin receptors and pain. J Pain, 10 (1): 4-28. [PMID:19111868]
Kirkby, NS; Hadoke, PW; Bagnall, AJ; Webb, DJ. (2008) The endothelin system as a therapeutic target in cardiovascular disease: great expectations or bleak house?. Br. J. Pharmacol., 153 (6): 1105-19. [PMID:17965745]
Kohan, DE; Rossi, NF; Inscho, EW; Pollock, DM. (2011) Regulation of blood pressure and salt homeostasis by endothelin. Physiol. Rev., 91 (1): 1-77. [PMID:21248162]
Nguyen, A; Thorin-Trescases, N; Thorin, E. (2010) Working under pressure: coronary arteries and the endothelin system. Am. J. Physiol. Regul. Integr. Comp. Physiol., 298 (5): R1188-94. [PMID:20237301]
Schneider, M. P., Boesen, E. I. and Pollock, D. M. (2007) Contrasting Actions of Endothelin ET(A) and ET(B) Receptors in Cardiovascular Disease. Annu Rev Pharmacol Toxicol, 47: 731–59. [PMID:17002597]
Schorlemmer, A; Matter, ML; Shohet, RV. (2008) Cardioprotective signaling by endothelin. Trends Cardiovasc. Med., 18 (7): 233-9. [PMID:19232951]
Thorin, E; Webb, DJ. (2010) Endothelium-derived endothelin-1. Pflugers Arch., 459 (6): 951-8. [PMID:19967386]
Virdis, A; Ghiadoni, L; Taddei, S. (2010) Human endothelial dysfunction: EDCFs. Pflugers Arch., 459 (6): 1015-23. [PMID:20107832]
Watts, SW. (2010) Endothelin receptors: what's new and what do we need to know?. Am. J. Physiol. Regul. Integr. Comp. Physiol., 298 (2): R254-60. [PMID:19907001]
1. Bolli, MH; Marfurt, J; Grisostomi, C; Boss, C; Binkert, C; Hess, P; Treiber, A; Thorin, E; Morrison, K; Buchmann, S; et al.. (2004) Novel benzo[1,4]diazepin-2-one derivatives as endothelin receptor antagonists. J. Med. Chem., 47 (11): 2776-95. [PMID:15139756]
2. 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]
3. Davenport, A. P. (2002) International Union of Pharmacology. XXIX. Update on endothelin receptor nomenclature. . Pharmacol. Rev., 54: 219-226. [PMID:12037137]
4. Davenport, A. P., Kuc, R. E., Ashby, M. J., Patt, W. C. and Doherty, A. M. (1998) Characterization of [125I]-PD164333, an ETA-selective non-peptide radiolabelled antagonist, in normal and diseased human tissues. Br. J. Pharmacol., 123: 223-230. [PMID:9489609]
5. Davenport, A. P., Kuc, R. E., Fitzgerald, F., Maguire, J. J., Berryman, K. and Doherty, A. M. (1994) [125I]-PD15242, a selective radioligand for human ETAreceptors. Br. J. Pharmacol., 111: 4-6. [PMID:8012722]
6. Harland, S. P., Kuc, R. E., Pickard, J. D. and Davenport, A. P. (1995) Characterization of endothelin receptors in human brain cortex, gliomas, and meningiomas. J. Cardiovasc. Pharmacol., 26: S408-S411. [PMID:8587429]
7. Hatae, N; Aksentijevich, N; Zemkova, HW; Kretschmannova, K; Tomic, M; Stojilkovic, SS. (2007) Cloning and functional identification of novel endothelin receptor type A isoforms in pituitary. Mol. Endocrinol., 21 (5): 1192-204. [PMID:17312275]
8. 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]
9. Kuc, R. E., Karet, F. E. and Davenport, A. P. (1995) Characterization of peptide and nonpeptide antagonists in human kidney. J. Cardiovasc. Pharmacol., 26: S373-S375. [PMID:8587419]
10. Maguire, J. J. and Davenport, A. P. (1995) ETA receptor-mediated constrictor responses to endothelin peptides in human blood vessels in vitro. Br. J. Pharmacol., 115: 191-197. [PMID:7647976]
11. Maguire, J. J., Kuc, R. E. and Davenport, A. P. (1997) Affinity and selectivity of PD156707, a novel nonpeptide endothelin antagonist, for human ET(A) and ET(B) receptors. . J. Pharmacol. Exp. Ther., 280: 1102-1108. [PMID:9023329]
12. 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: 1427-1430. [PMID:9113361]
13. Molenaar, P., Kuc, R. E. and Davenport, A. P. (1992) Characterization of two new ETBselective radioligands, [125I]-BQ3020 and [125I]-[Ala1,3,11,15]ET-1 in human heart. Br. J. Pharmacol., 107: 637-639. [PMID:1472961]
14. Morris, CD; Rose, A; Curwen, J; Hughes, AM; Wilson, DJ; Webb, DJ. (2005) Specific inhibition of the endothelin A receptor with ZD4054: clinical and pre-clinical evidence. Br. J. Cancer, 92 (12): 2148-52. [PMID:15956965]
15. 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: 202-207. [PMID:8301559]
16. Ohlstein, E. H., Nambi, P., Hay, D. W., Gellai, M., Brooks, D. P., Luengo, J., Xiang, J. N. and Elliott, J. D. (1998) Nonpeptide endothelin receptor antagonists. XI. Pharmacological characterization of SB 234551, a high affinity nonpeptide ETAreceptor antagonist. J. Pharmacol. Exp. Ther., 286: 650-656. [PMID:9694916]
17. Opgenorth, T. J., Adler, A. L., Calzadilla, S. V., Chiou, W. J., Dayton, B. D., Dixon, D. B., Gehrke, L. J., Hernandez, L., Magnuson, S. R., Marsh, K. C., Novosad, E. I., Von Geldern, T. W., Wessale, J. L., Winn, M. and Wu-Wong, J. R. (1996) Pharmacological Characterization of A-127722, an orally active and highly potent ETA-selective receptor antagonist. J. Pharmacol. Exp. Ther., 276: 473-481. [PMID:8632312]
18. Peter, M. G. and Davenport, A. P. (1996) Characterization of the endothelin receptor selective agonist, BQ3020 and antagonists BQ123, FR139317, BQ788, 50235, Ro462005 and bosentan in the heart. Br J Pharmacol., 117: 455-462. [PMID:7881728]
19. Reynolds, EE; Hwang, O; Flynn, MA; Welch, KM; Cody, WL; Steinbaugh, B; He, JX; Chung, FZ; Doherty, AM. (1995) Pharmacological differences between rat and human endothelin B receptors. Biochem. Biophys. Res. Commun., 209 (2): 506-12. [PMID:7733918]
20. Riechers, H; Albrecht, HP; Amberg, W; Baumann, E; Bernard, H; Böhm, HJ; Klinge, D; Kling, A; Müller, S; Raschack, M; et al.. (1996) Discovery and optimization of a novel class of orally active nonpeptidic endothelin-A receptor antagonists. J. Med. Chem., 39 (11): 2123-8. [PMID:8667356]
21. Russell, F. D. and Davenport, A. P. (1996) Characterization of the binding of endothelin ETB selective ligands in human and rat heart. Br. J. Pharmacol., 119: 631-636. [PMID:8904635]
22. von Geldern, T. W., Tasker, A. S., Sorensen, B. K., Winn, M., Szczepankiewicz, B. G., Dixon, D. B., Chiou, W. J., Wang, L., Wessale, J. L., Adler, A., Marsh, K. C., Nguyen, B. and Opgenorth, T. J. (1999) Pyrrolidine-3-carboxylic acids as endothelin antagonists. 4. Side chain conformational restriction leads to ETBselectivity. J. Med. Chem., 42: 3668-3678. [PMID:10479298]
23. Watakabe, T; Urade, Y; Takai, M; Umemura, I; 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 (3): 867-73. [PMID:1320877]
24. Wu, C; Chan, MF; Stavros, F; Raju, B; Okun, I; Mong, S; Keller, KM; Brock, T; Kogan, TP; Dixon, RA. (1997) Discovery of TBC11251, a potent, long acting, orally active endothelin receptor-A selective antagonist. J. Med. Chem., 40 (11): 1690-7. [PMID:9171878]
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Subtypes of the ETB receptor have been proposed, although gene disruption studies in mice suggest that the heterogeneity results from a single gene product [12].