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. 1993 Nov;110(3):1175–1183. doi: 10.1111/j.1476-5381.1993.tb13938.x

Endothelin receptor subtypes in human and guinea-pig pulmonary tissues.

D W Hay 1, M A Luttmann 1, W C Hubbard 1, B J Undem 1
PMCID: PMC2175787  PMID: 8298806

Abstract

1. In this study the endothelin (ET) receptor subtypes mediating contractions produced by ET-1 in human and guinea-pig pulmonary tissues were investigated. In addition the receptor responsible for ET-1-induced prostanoid release in human bronchus was determined. 2. In human bronchus and human pulmonary artery ET-1 (0.1 nM-0.3 microM) was a potent and effective contractile agent (pD2 = 7.58 +/- 0.15, n = 6, and 8.48 +/- 0.11, n = 7, respectively). BQ-123 (1-10 microM), a potent and selective ETA receptor antagonist, potently antagonized ET-1-induced contraction in human pulmonary artery (pKB = 6.8 with 1 microM BQ-123, n = 7) but had no effect in human bronchus (n = 6). 3. Sarafotoxin S6c (0.1 nM-0.1 microM), the ETB-selective agonist, did not contract human pulmonary artery (n = 5), but potently and effectively contracted human bronchus: pD2 = 8.41 +/- 0.17, maximum response = 74.4 +/- 3.1% of 10 microM carbachol; n = 5. BQ-123 (1-10 microM) did not antagonize sarafotoxin S6c-induced contraction in human bronchus (n = 5). 4. ET-1 potently contracted guinea-pig trachea, bronchus, pulmonary artery and aorta (pD2 = 8.15 +/- 0.14, 7.72 +/- 0.12, 8.52 +/- 0.12, and 8.18 +/- 0.12, respectively, n = 6-14).(ABSTRACT TRUNCATED AT 250 WORDS)

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Selected References

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  1. Abraham W. M., Ahmed A., Cortes A., Spinella M. J., Malik A. B., Andersen T. T. A specific endothelin-1 antagonist blocks inhaled endothelin-1-induced bronchoconstriction in sheep. J Appl Physiol (1985) 1993 May;74(5):2537–2542. doi: 10.1152/jappl.1993.74.5.2537. [DOI] [PubMed] [Google Scholar]
  2. Advenier C., Sarria B., Naline E., Puybasset L., Lagente V. Contractile activity of three endothelins (ET-1, ET-2 and ET-3) on the human isolated bronchus. Br J Pharmacol. 1990 May;100(1):168–172. doi: 10.1111/j.1476-5381.1990.tb12071.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  3. Arai H., Hori S., Aramori I., Ohkubo H., Nakanishi S. Cloning and expression of a cDNA encoding an endothelin receptor. Nature. 1990 Dec 20;348(6303):730–732. doi: 10.1038/348730a0. [DOI] [PubMed] [Google Scholar]
  4. Brink C., Gillard V., Roubert P., Mencia-Huerta J. M., Chabrier P. E., Braquet P., Verley J. Effects and specific binding sites of endothelin in human lung preparations. Pulm Pharmacol. 1991;4(1):54–59. doi: 10.1016/0952-0600(91)90040-a. [DOI] [PubMed] [Google Scholar]
  5. Cardell L. O., Uddman R., Edvinsson L. A novel ETA-receptor antagonist, FR 139317, inhibits endothelin-induced contractions of guinea-pig pulmonary arteries, but not trachea. Br J Pharmacol. 1993 Feb;108(2):448–452. doi: 10.1111/j.1476-5381.1993.tb12824.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  6. Cardell L. O., Uddman R., Edvinsson L. Evidence for multiple endothelin receptors in the guinea-pig pulmonary artery and trachea. Br J Pharmacol. 1992 Feb;105(2):376–380. doi: 10.1111/j.1476-5381.1992.tb14261.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  7. Cernacek P., Stewart D. J. Immunoreactive endothelin in human plasma: marked elevations in patients in cardiogenic shock. Biochem Biophys Res Commun. 1989 Jun 15;161(2):562–567. doi: 10.1016/0006-291x(89)92636-3. [DOI] [PubMed] [Google Scholar]
  8. D'Orléans-Juste P., Télémaque S., Claing A., Ihara M., Yano M. Human big-endothelin-1 and endothelin-1 release prostacyclin via the activation of ET1 receptors in the rat perfused lung. Br J Pharmacol. 1992 Apr;105(4):773–775. doi: 10.1111/j.1476-5381.1992.tb09055.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  9. Filep J. G., Battistini B., Côté Y. P., Beaudoin A. R., Sirois P. Endothelin-1 induces prostacyclin release from bovine aortic endothelial cells. Biochem Biophys Res Commun. 1991 May 31;177(1):171–176. doi: 10.1016/0006-291x(91)91964-e. [DOI] [PubMed] [Google Scholar]
  10. Hagiwara H., Nagasawa T., Lodhi K. M., Kozuka M., Ito T., Hirose S. Affinity chromatographic purification of bovine lung endothelin receptor using biotinylated endothelin and avidin-agarose. J Chromatogr. 1992 Apr 24;597(1-2):331–334. doi: 10.1016/0021-9673(92)80128-h. [DOI] [PubMed] [Google Scholar]
  11. Harrison V. J., Randriantsoa A., Schoeffter P. Heterogeneity of endothelin-sarafotoxin receptors mediating contraction of pig coronary artery. Br J Pharmacol. 1992 Mar;105(3):511–513. doi: 10.1111/j.1476-5381.1992.tb09009.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  12. Hay D. W., Henry P. J., Goldie R. G. Endothelin and the respiratory system. Trends Pharmacol Sci. 1993 Jan;14(1):29–32. doi: 10.1016/0165-6147(93)90111-v. [DOI] [PubMed] [Google Scholar]
  13. Hay D. W. Pharmacological evidence for distinct endothelin receptors in guinea-pig bronchus and aorta. Br J Pharmacol. 1992 Aug;106(4):759–761. doi: 10.1111/j.1476-5381.1992.tb14407.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  14. Hemsén A., Franco-Cereceda A., Matran R., Rudehill A., Lundberg J. M. Occurrence, specific binding sites and functional effects of endothelin in human cardiopulmonary tissue. Eur J Pharmacol. 1990 Dec 4;191(3):319–328. doi: 10.1016/0014-2999(90)94164-s. [DOI] [PubMed] [Google Scholar]
  15. Henry P. J., Rigby P. J., Self G. J., Preuss J. M., Goldie R. G. Relationship between endothelin-1 binding site densities and constrictor activities in human and animal airway smooth muscle. Br J Pharmacol. 1990 Aug;100(4):786–792. doi: 10.1111/j.1476-5381.1990.tb14093.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  16. Hubbard W. C., Litterst C. L., Liu M. C., Bleecker E. R., Eggleston J. C., McLemore T. L., Boyd M. R. Profiling of prostaglandin biosynthesis in biopsy fragments of human lung carcinomas and normal human lung by capillary gas chromatography-negative ion chemical ionization mass spectrometry. Prostaglandins. 1986 Dec;32(6):889–906. doi: 10.1016/0090-6980(86)90097-3. [DOI] [PubMed] [Google Scholar]
  17. Ihara M., Noguchi K., Saeki T., Fukuroda T., Tsuchida S., Kimura S., Fukami T., Ishikawa K., Nishikibe M., Yano M. Biological profiles of highly potent novel endothelin antagonists selective for the ETA receptor. Life Sci. 1992;50(4):247–255. doi: 10.1016/0024-3205(92)90331-i. [DOI] [PubMed] [Google Scholar]
  18. Inoue A., Yanagisawa M., Kimura S., Kasuya Y., Miyauchi T., Goto K., Masaki T. The human endothelin family: three structurally and pharmacologically distinct isopeptides predicted by three separate genes. Proc Natl Acad Sci U S A. 1989 Apr;86(8):2863–2867. doi: 10.1073/pnas.86.8.2863. [DOI] [PMC free article] [PubMed] [Google Scholar]
  19. Kloog Y., Ambar I., Sokolovsky M., Kochva E., Wollberg Z., Bdolah A. Sarafotoxin, a novel vasoconstrictor peptide: phosphoinositide hydrolysis in rat heart and brain. Science. 1988 Oct 14;242(4876):268–270. doi: 10.1126/science.2845579. [DOI] [PubMed] [Google Scholar]
  20. Kloog Y., Bousso-Mittler D., Bdolah A., Sokolovsky M. Three apparent receptor subtypes for the endothelin/sarafotoxin family. FEBS Lett. 1989 Aug 14;253(1-2):199–202. doi: 10.1016/0014-5793(89)80958-5. [DOI] [PubMed] [Google Scholar]
  21. Kloog Y., Sokolovsky M. Similarities in mode and sites of action of sarafotoxins and endothelins. Trends Pharmacol Sci. 1989 Jun;10(6):212–214. doi: 10.1016/0165-6147(89)90261-7. [DOI] [PubMed] [Google Scholar]
  22. Kozuka M., Ito T., Hirose S., Lodhi K. M., Hagiwara H. Purification and characterization of bovine lung endothelin receptor. J Biol Chem. 1991 Sep 5;266(25):16892–16896. [PubMed] [Google Scholar]
  23. Maggi C. A., Giuliani S., Patacchini R., Santicioli P., Rovero P., Giachetti A., Meli A. The C-terminal hexapeptide, endothelin-(16-21), discriminates between different endothelin receptors. Eur J Pharmacol. 1989 Jul 4;166(1):121–122. doi: 10.1016/0014-2999(89)90693-6. [DOI] [PubMed] [Google Scholar]
  24. Martin E. R., Brenner B. M., Ballermann B. J. Heterogeneity of cell surface endothelin receptors. J Biol Chem. 1990 Aug 15;265(23):14044–14049. [PubMed] [Google Scholar]
  25. Masaki T., Yanagisawa M., Goto K. Physiology and pharmacology of endothelins. Med Res Rev. 1992 Jul;12(4):391–421. doi: 10.1002/med.2610120405. [DOI] [PubMed] [Google Scholar]
  26. Masuda Y., Miyazaki H., Kondoh M., Watanabe H., Yanagisawa M., Masaki T., Murakami K. Two different forms of endothelin receptors in rat lung. FEBS Lett. 1989 Nov 6;257(2):208–210. doi: 10.1016/0014-5793(89)81535-2. [DOI] [PubMed] [Google Scholar]
  27. Mattoli S., Soloperto M., Marini M., Fasoli A. Levels of endothelin in the bronchoalveolar lavage fluid of patients with symptomatic asthma and reversible airflow obstruction. J Allergy Clin Immunol. 1991 Sep;88(3 Pt 1):376–384. doi: 10.1016/0091-6749(91)90100-3. [DOI] [PubMed] [Google Scholar]
  28. Nakamichi K., Ihara M., Kobayashi M., Saeki T., Ishikawa K., Yano M. Different distribution of endothelin receptor subtypes in pulmonary tissues revealed by the novel selective ligands BQ-123 and [Ala1,3,11,15]ET-1. Biochem Biophys Res Commun. 1992 Jan 15;182(1):144–150. doi: 10.1016/s0006-291x(05)80123-8. [DOI] [PubMed] [Google Scholar]
  29. Panek R. L., Major T. C., Hingorani G. P., Doherty A. M., Taylor D. G., Rapundalo S. T. Endothelin and structurally related analogs distinguish between endothelin receptor subtypes. Biochem Biophys Res Commun. 1992 Mar 16;183(2):566–571. doi: 10.1016/0006-291x(92)90519-q. [DOI] [PubMed] [Google Scholar]
  30. Payne A. N., Whittle B. J. Potent cyclo-oxygenase-mediated bronchoconstrictor effects of endothelin in the guinea-pig in vivo. Eur J Pharmacol. 1988 Dec 13;158(3):303–304. doi: 10.1016/0014-2999(88)90085-4. [DOI] [PubMed] [Google Scholar]
  31. Pons F., Boichot E., Lagente V., Touvay C., Mencia-Huerta J. M., Braquet P. Role of endothelin in pulmonary function. Pulm Pharmacol. 1992 Sep;5(3):213–219. doi: 10.1016/0952-0600(92)90043-g. [DOI] [PubMed] [Google Scholar]
  32. Sakamoto A., Yanagisawa M., Sakurai T., Takuwa Y., Yanagisawa H., Masaki T. Cloning and functional expression of human cDNA for the ETB endothelin receptor. Biochem Biophys Res Commun. 1991 Jul 31;178(2):656–663. doi: 10.1016/0006-291x(91)90158-4. [DOI] [PubMed] [Google Scholar]
  33. Sakurai T., Yanagisawa M., Masaki T. Molecular characterization of endothelin receptors. Trends Pharmacol Sci. 1992 Mar;13(3):103–108. doi: 10.1016/0165-6147(92)90038-8. [DOI] [PubMed] [Google Scholar]
  34. Sakurai T., Yanagisawa M., Takuwa Y., Miyazaki H., Kimura S., Goto K., Masaki T. Cloning of a cDNA encoding a non-isopeptide-selective subtype of the endothelin receptor. Nature. 1990 Dec 20;348(6303):732–735. doi: 10.1038/348732a0. [DOI] [PubMed] [Google Scholar]
  35. Samson W. K., Skala K. D., Alexander B. D., Huang F. L. Pituitary site of action of endothelin: selective inhibition of prolactin release in vitro. Biochem Biophys Res Commun. 1990 Jun 15;169(2):737–743. doi: 10.1016/0006-291x(90)90393-2. [DOI] [PubMed] [Google Scholar]
  36. Schvartz I., Ittoop O., Hazum E. Direct evidence for multiple endothelin receptors. Biochemistry. 1991 May 28;30(21):5325–5327. doi: 10.1021/bi00235a028. [DOI] [PubMed] [Google Scholar]
  37. Similarity of endothelin to snake venom toxin. Nature. 1988 Sep 22;335(6188):303–303. doi: 10.1038/335303a0. [DOI] [PubMed] [Google Scholar]
  38. Similarity of endothelin to snake venom toxin. Nature. 1988 Sep 22;335(6188):303–303. doi: 10.1038/335303a0. [DOI] [PubMed] [Google Scholar]
  39. Springall D. R., Howarth P. H., Counihan H., Djukanovic R., Holgate S. T., Polak J. M. Endothelin immunoreactivity of airway epithelium in asthmatic patients. Lancet. 1991 Mar 23;337(8743):697–701. doi: 10.1016/0140-6736(91)90279-x. [DOI] [PubMed] [Google Scholar]
  40. Takasaki C., Tamiya N., Bdolah A., Wollberg Z., Kochva E. Sarafotoxins S6: several isotoxins from Atractaspis engaddensis (burrowing asp) venom that affect the heart. Toxicon. 1988;26(6):543–548. doi: 10.1016/0041-0101(88)90234-6. [DOI] [PubMed] [Google Scholar]
  41. Takayanagi R., Ohnaka K., Takasaki C., Ohashi M., Nawata H. Multiple subtypes of endothelin receptors in porcine tissues: characterization by ligand binding, affinity labeling and regional distribution. Regul Pept. 1991 Jan 1;32(1):23–37. doi: 10.1016/0167-0115(91)90004-z. [DOI] [PubMed] [Google Scholar]
  42. Tschirhart E. J., Drijfhout J. W., Pelton J. T., Miller R. C., Jones C. R. Endothelins: functional and autoradiographic studies in guinea pig trachea. J Pharmacol Exp Ther. 1991 Jul 1;258(1):381–387. [PubMed] [Google Scholar]
  43. Urade Y., Fujitani Y., Oda K., Watakabe T., Umemura I., Takai M., Okada T., Sakata K., Karaki H. An endothelin B receptor-selective antagonist: IRL 1038, [Cys11-Cys15]-endothelin-1(11-21) FEBS Lett. 1992 Oct 12;311(1):12–16. doi: 10.1016/0014-5793(92)81355-p. [DOI] [PubMed] [Google Scholar]
  44. VAN ROSSUM J. M. Cumulative dose-response curves. II. Technique for the making of dose-response curves in isolated organs and the evaluation of drug parameters. Arch Int Pharmacodyn Ther. 1963;143:299–330. [PubMed] [Google Scholar]
  45. Watanabe H., Miyazaki H., Kondoh M., Masuda Y., Kimura S., Yanagisawa M., Masaki T., Murakami K. Two distinct types of endothelin receptors are present on chick cardiac membranes. Biochem Biophys Res Commun. 1989 Jun 30;161(3):1252–1259. doi: 10.1016/0006-291x(89)91377-6. [DOI] [PubMed] [Google Scholar]
  46. Williams D. L., Jr, Jones K. L., Colton C. D., Nutt R. F. Identification of high affinity endothelin-1 receptor subtypes in human tissues. Biochem Biophys Res Commun. 1991 Oct 31;180(2):475–480. doi: 10.1016/s0006-291x(05)81089-7. [DOI] [PubMed] [Google Scholar]
  47. Williams D. L., Jr, Jones K. L., Pettibone D. J., Lis E. V., Clineschmidt B. V. Sarafotoxin S6c: an agonist which distinguishes between endothelin receptor subtypes. Biochem Biophys Res Commun. 1991 Mar 15;175(2):556–561. doi: 10.1016/0006-291x(91)91601-8. [DOI] [PubMed] [Google Scholar]
  48. Wollberg Z., Bdolah A., Kochva E. Vasoconstrictor effects of sarafotoxins in rabbit aorta: structure-function relationships. Biochem Biophys Res Commun. 1989 Jul 14;162(1):371–376. doi: 10.1016/0006-291x(89)92006-8. [DOI] [PubMed] [Google Scholar]
  49. 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. 1988 Mar 31;332(6163):411–415. doi: 10.1038/332411a0. [DOI] [PubMed] [Google Scholar]
  50. Yanagisawa M., Masaki T. Endothelin, a novel endothelium-derived peptide. Pharmacological activities, regulation and possible roles in cardiovascular control. Biochem Pharmacol. 1989 Jun 15;38(12):1877–1883. doi: 10.1016/0006-2952(89)90484-x. [DOI] [PubMed] [Google Scholar]
  51. Yanagisawa M., Masaki T. Molecular biology and biochemistry of the endothelins. Trends Pharmacol Sci. 1989 Sep;10(9):374–378. doi: 10.1016/0165-6147(89)90011-4. [DOI] [PubMed] [Google Scholar]

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