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Radioligand binding assays and quantitative autoradiography of endothelin receptors

  • Anthony P. Davenport
  • Rhoda E. Kuc
Protocol
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Part of the Methods in Molecular Biology™ book series (MIMB, volume 206)

Abstract

Endothelin (ET) receptors belong to the G-protein-linked seven transmembrane spanning family of receptors, located in the plasma membrane. Receptors can be identified by their amino acid structure and provide unambiguous evidence for expression of a gene encoding a particular sub-type in specific cells or tissues (see  Chapter 6).

Keywords

Quantitative Autoradiography Competition Binding Assay Unlabeled Ligand Saturation Assay Ligand Program 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

References

  1. 1.
    Arai H., Hori S., Aramori I., Ohkubo H., and Nakanishi S. (1990) Cloning and expression of a cDNA encoding an endothelin receptor. Nature 348, 730–732.PubMedCrossRefGoogle Scholar
  2. 2.
    Sakurai T., Yanagisawa M., Takuwa Y., Miyazaki H., Kimura S., Goto K., and Masaki T. (1990) Cloning of a cDNA encoding a nonisopeptide-selective subtype of the endothelin receptor. Nature 348, 732–735.PubMedCrossRefGoogle Scholar
  3. 3.
    Davenport A.P. (2000) Endothelin receptors. Iuphar Compendium of Receptor Characterisation and Classification, 2nd edition. Iuphar Media London, UK. 182–188.Google Scholar
  4. 4.
    Davenport A.P., O’Reilly G., Molenaar P., Maguire J.J. Kuc R.E., Sharkey A., Bacon C.R., and Ferro A. (1993) Human endothelin receptors characterized using reverse transcriptase-polymerase chain reaction, in situ hybridization and sub-type selective ligands BQ123 and BQ3020:Evidence for expression of ETB receptors in human vascular smooth muscle. J. Cardiovasc. Pharmacol. 22(S8), 22–25.CrossRefGoogle Scholar
  5. 5.
    Molenaar P., O’ Reilly G., Sharkey A., Kuc R.E., Harding D.P., Plumpton P., Gresham G.A., and Davenport A.P. (1993) Characterization and localization of endothelin receptor sub-types in the human atrio-ventricular conducting system and myocardium. Circ. Res. 72, 526–538.PubMedGoogle Scholar
  6. 6.
    Telemaque-Potts S., Kuc R.E., Yanagisawa M., and Davenport A.P. (2000) Tissue-specific modulation of endothelin receptors in a rat model of hyperten-sion. J. Cardiovasc. Pharmacol. 36(S1), 122–123.Google Scholar
  7. 7.
    Kuc R.E. and Davenport A.P. (2000) Endothelin-A-receptors in human aorta and pulmonary arteries are down regulated in patients with cardiovascular disease:An adaptive response to increased levels of ET-1?J. Cardiovasc. Pharmacol. 36(S1), 377–379.Google Scholar
  8. 8.
    Keen M. (ed.) (1999) Receptor Binding Techniques. Humana Press Totowa, NJ.Google Scholar
  9. 9.
    Hulme E. (1992) Receptor-Ligand Interactions. IRL Oxford, UK.Google Scholar
  10. 10.
    Kenakin T. (1993) Pharmacologic Analysis of Drug-Receptor Interactions. Raven Press New York, USA.Google Scholar
  11. 11.
    Davenport A.P. and Russell F.D. (2001) Endothelin converting enzymes and endothelin receptor localisation in human tissues, in Handbook of Experimen-tal Pharmacology, vol. 152 (Warner T.D. ed.), Springer-Verlag Berlin, Ger-many, pp. 209–237.Google Scholar
  12. 12.
    Davenport A.P. (1997) Distribution of endothelin receptors, in Endothelins in Biology and Medicine (Miller R., Pelton J.T., and Huggins J., eds.), CRC Press Inc Florida. pp. 45–68.Google Scholar
  13. 13.
    Davenport A.P., O’ Reilly G., and Kuc R.E. (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, 1110–1116.PubMedGoogle Scholar
  14. 14.
    Davenport A.P. and Maguire J.J. (1994) Endothelin-induced vasoconstriction is mediated by ETA receptors in man. Trends Pharmacol. Sci. 15, 136–137.CrossRefGoogle Scholar
  15. 15.
    Gray G.A. and Webb D.J. (1996) The endothelin system and its potential as a therapeutic target in cardiovascular disease. Pharmacol. Ther. 72, 109–148.PubMedCrossRefGoogle Scholar
  16. 16.
    Douglas S.A. and Ohlstein E.H. (1997) Signal transduction mechanisms mediating the vascular actions of endothelin. J. Vasc. Res. 34, 152–64.PubMedCrossRefGoogle Scholar
  17. 17.
    Henry P.J. and Goldie R.G. (2001) Endothelin receptors, in Handbook of Experi-mental Pharmacology, vol. 152 (Warner T.D., ed), Springer-Verlag Berlin, Germany, pp. 69–114.Google Scholar
  18. 18.
    Stanimirovic D.B., Yamamoto T., Uematsu S., and Spatz M. (1994) Endothelin-1 receptor binding and cellular signal transduction in cultured human brain endothelial cells. J. Neurochem. 62, 592–601.PubMedCrossRefGoogle Scholar
  19. 19.
    Zhang Y.F., Jeffery S., Burchill S.A., Berry P.A., Kaski J.C. and Carter N.D. (1998) Truncated human endothelin receptor A produced by alternative splicing and its expression in melanoma. Br. J. Cancer 78, 1141–1146.PubMedCrossRefGoogle Scholar
  20. 20.
    Shyamala V., Moulthrop T.H., Stratton Thomas J., and Tekamp Olson P. (1994) Two distinct human endothelin B receptors generated by alternative splic-ing from a single gene. Cell Mol. Biol. Res. 40, 285–296.PubMedGoogle Scholar
  21. 21.
    Elshourbagy N.A., Adamou J.E., Gagnon A.W., Wu H.L., Pullen M., and Nambi P. (1996) Molecular characterization of a novel human endothelin recep-tor splice variant. J. Biol. Chem. 271, 25,300–25,307.PubMedCrossRefGoogle Scholar
  22. 22.
    Mizuguchi T., Nishiyama M., Moroi K., Tanaka H., Saito T., Masuda Y., et al. (1997) Analysis of two pharmacologically predicted endothelin B receptor sub-types by using the endothelin B receptor gene knockout mouse. Br. J. Pharmacol. 120, 1427–1430.PubMedCrossRefGoogle Scholar
  23. 23.
    Molenaar P., Kuc R.E., and Davenport A.P. (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, 637–639.PubMedGoogle Scholar
  24. 24.
    Davenport A.P., Kuc R.E., Hoskins S.L., Karet F.E., and Fitzgerald F. (1994) [125I]-PD151242:a selective ligand for endothelin ETA receptors in human kidney which localizes to renal vasculature. Brit. J. Pharmacol. 113, 1303–1310.Google Scholar
  25. 25.
    Peter M.G. and Davenport A.P. (1996) Characterisation of endothelin receptor selective agonist BQ3020 and antagonists BQ123, FR139317, BQ788, 50235, Ro462005 and bosentan in the heart. Brit. J. Pharmacol. 117, 455–462.Google Scholar
  26. 26.
    Russell F.D. and Davenport A.P. (1996) Characterisation of the binding of endothelin ETB selective ligands in human and rat heart. Brit. J. Pharmacol. 119, 631–636.Google Scholar
  27. 27.
    Flynn M.A., Haleen S.J., Welch K.M., Cheng X.M., and Reynolds E.E. (1998) Endothelin B receptors on human endothelial and smooth-muscle cells show equivalent binding pharmacology. J. Cardiovasc. Pharmacol. 32, 106–116.PubMedCrossRefGoogle Scholar
  28. 28.
    Lecoin L., Sakurai T., Ngo M.T., Abe Y., Yanagisawa M., and Le-Douarin N.M. (1998) Cloning and characterization of a novel endothelin receptor subtype in the avian class. Proc. Natl. Acad. Sci. 95, 3024–3029.PubMedCrossRefGoogle Scholar
  29. 29.
    Karne S., Jayawickreme C.K., and Lerner M.R. (1993) Cloning and character-ization of an endothelin-3 specific receptor (ETC receptor) from Xenopus laevis dermal melanophores. J. Biol. Chem. 268, 19126–19133.PubMedGoogle Scholar
  30. 30.
    Davenport A.P. and Morton A.J. (1991) Binding sites for 125I-125I ET-1, ET-2, ET-3 and vasoactive intestinal contractor are present in adult rat brain and neurone-enriched primary cultures of embryonic brain cells. Brain Res. 554, 278–285.PubMedCrossRefGoogle Scholar
  31. 31.
    Bacon C.R.and Davenport A.P. (1996) Endothelin receptors in human coronary artery and aorta. Brit. J. Pharmacol. 117, 986–992.Google Scholar
  32. 32.
    Maguire J.J., Kuc R.E., Rous B.A., and Davenport A.P. (1996) Failure of BQ123, a more potent antagonist of sarafotoxin S6b than of endothelin-1, to dis-tinguish between these agonists in binding experiments. Brit. J. Pharmacol. 118, 355–342.Google Scholar
  33. 33.
    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 ETA receptors. Br. J. Pharmacol. 111, 4–6.PubMedGoogle Scholar
  34. 34.
    Davenport A.P., Kuc R.E., Ashby M.J., Patt W.C., and Doherty A.M. (1998) Characterisation of [125I ]-PD164333, an ETA-selective nonpeptide radiolabeled antagonist, in normal and diseased human tissues. Br. J. Pharmacol. 123, 223–230.PubMedCrossRefGoogle Scholar
  35. 35.
    Ihara M., Yamanaka R., Ohwaki K., Ozaki S., Fukami T., Ishikawa K., et al. (1995) [3H]-BQ-123, a highly specific and reversible radioligand for the endothelin ETA receptor subtype. Eur. J. Pharmacol. 274, 1–6.PubMedCrossRefGoogle Scholar
  36. 36.
    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]-IRL1620. Biochem. Biophys. Res. Commun. 185, 867–873.PubMedCrossRefGoogle Scholar
  37. 37.
    Ihara M., Noguchi K., Saeki T., Fukuroda T., Tsuchida S., Kimura S., et al. (1992) Biological profiles of highly potent novel endothelin antagonists selective for the ET(A)receptor. Life Sci. 50, 247–255.PubMedCrossRefGoogle Scholar
  38. 38.
    Aramori I., Nirei H., Shoubo M., Sogabe K., Nakamura K., Kojo H., et al. (1993) Subtype selectivity of a novel endothelin antagonist, FR139317, for the two endothelin receptors in transfected Chinese hamster ovary cells. Mol. Pharmacol. 43, 127–131.PubMedGoogle Scholar
  39. 39.
    William D.L., Jr., Jones K.L., Pettibone D.J., Lis E.V., and Clineschmidt B. V. (1991) Sarafotoxin S6c, an agonist which distinguishes between endothelin receptor subtypes. Biochem. Biophys. Res Commun. 175, 556–561.CrossRefGoogle Scholar
  40. 40.
    Ishikawa K., Ihara M., Noguchi K., Mase T., Mino N., Saeki T., et al. (1994) Biochemical and pharmacological profile of a potent and selective endothelin B-receptor antagonist, BQ-788. Proc. Natl. Acad. Sci. USA 91, 4892–4896.PubMedCrossRefGoogle Scholar
  41. 41.
    Battistini B. and Dussault P. (1998) Blocking of the endothelin system:the development of receptor antagonists. Pulm. Pharmacol. Ther. 11, 97–112.PubMedCrossRefGoogle Scholar
  42. 42.
    Peter M.G. and Davenport A.P. (1995) Selectivity of [125I]-PD151242 for the human, rat and porcine endothelin ETA receptors in the heart. Brit. J. Pharmacol. 114, 297–302.Google Scholar
  43. 43.
    Munson P.J. and Rodbard D. (1980) Ligand:a versatile computerized approach for characterization of ligand-binding systems. Anal. Biochem. 107, 220–239.PubMedCrossRefGoogle Scholar
  44. 44.
    McPherson G.A. (1985) Analysis of radioligand binding experiments. A collection of computer programs for the IBM PC. J. Pharmacol. Meth. 14, 213–228.CrossRefGoogle Scholar
  45. 45.
    Davenport A.P. and Hall M.D. (1988) Comparison between brain paste and polymer standards for quantitative receptor autoradiography. J. Neurosci. Meth. 25, 75–82.CrossRefGoogle Scholar

Copyright information

© Humana Press Inc. 2002

Authors and Affiliations

  • Anthony P. Davenport
    • 1
  • Rhoda E. Kuc
    • 1
  1. 1.Clinical Pharmacology UnitUniversity of CambridgeCambridgeUK

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