Nonpeptide endothelin receptor antagonists. VII: Binding characteristics of [3H]SB 209670, a novel nonpeptide antagonist of endothelin receptors

Journal of Pharmacology and Experimental Therapeutics

Volumn 277, Issue 3, 1996, Pages 1567-1571

  Nambi, Ponnal ^a   Pullen, Mark ^a   Wu, Hsiao Ling ^a   Lee, Donna ^b   Saunders, David ^a   Heys, Richard ^a   Aiyar, Nambi ^a   Leber, Jack ^a   Elliott, John ^a   Brooks, David ^a   Ohlstein, Eliot ^a   Ruffolo, Robert ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

^b UW2521 ^*

Author keywords

[No Author keywords available]

Indexed keywords

3 (2 CARBOXYMETHOXY 4 METHOXYPHENYL) 1 (3,4 METHYLENEDIOXYPHENYL) 5 PROPOXY 2 INDANCARBOXYLIC ACID; BOSENTAN; CYCLO(DEXTRO TRYPTOPHYL DEXTRO ASPARTYLPROLYL DEXTRO VALYLLEUCYL); ENDOTHELIN 1; ENDOTHELIN 3; ENDOTHELIN A RECEPTOR; ENDOTHELIN B RECEPTOR; ENDOTHELIN RECEPTOR ANTAGONIST; N ACETYL 3,3 DIPHENYL DEXTRO ALANYLLEUCYLASPARTYLISOLEUCYLISOLEUCYLTRYPTOPHAN; RES 701 1; SARAFOTOXIN S6C; TRITIUM;

ANIMAL CELL; ARTICLE; CELL MEMBRANE; CHO CELL; CONTROLLED STUDY; DISSOCIATION CONSTANT; DRUG POTENCY; DRUG RECEPTOR BINDING; ISOTOPE LABELING; LIGAND BINDING; NONHUMAN; PRIORITY JOURNAL; RECEPTOR AFFINITY;

ANIMALS; BINDING, COMPETITIVE; CHO CELLS; CRICETINAE; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; INDANS; KINETICS; RADIOLIGAND ASSAY; RECEPTORS, ENDOTHELIN;

EID: 12644251994     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (26)

1. ARAI, H., HORI, S., ARAMORI, H., OHKUBO, H. AND NAKANISHI, S.: Cloning and expression of a cDNA encoding an endothelin receptor. Nature (Lond.) 348: 730-732, 1990.
2. BROOKS, D. P., DEPALMA, P. D., PULLEN, M. AND NAMBI, P.: Characterization of canine renal endothelin receptor subtypes and their function. J. Pharmacol. Exp. Ther. 268: 1091-1097, 1994.
3. CLOZEL, M., BREU, V., BURAJ, JC, CASSAL, J. H., FISCHLI, W., GRAY, G. A., HIRTH, G., LOFFLER, B. M., MULLER, M., NEIDHART, W. AND RAMUZ, H.: Pathological role of endothelin revealed by the first orally active endothelin receptor antagonist. Nature (Lond.) 365: 759-761, 1993.
4. CODY, W. L., DOHERTY, A. M., HE, J-X., DEPUE, P. L., RAPUNDALO, S. T., HINGORANI, G. A., MAJOR, T. C., PANEK, R. L., DUDLEY, D. T., HALEEM, S. J., LADOUCEUR, D., HILL, K. E., FLYNN, M. A. AND REYNOLDS, E. E.: Design of a functional hexapeptide antagonist of endothelin. J. Med. Chem. 35: 3301-3303, 1992.
5. ELLIOTT, J. D., LAGO, M. A., COUSINS, R. D., GAO, A., LEBER, J. D., ERHARD, K. F., NAMBI, P., ELSHOURBAGY, N., KUMAR, C., LEE, J. A., BEAN, J. W., DEBROSSE, C. W., EGGLESTON, D. S., BROOKS, D. P., FEUERSTEIN, G. F., RUFFOLO, JR., R. R., WEINSTOCK, J., GLEASON, J. G., PEISHOFF, C. E. AND OHLSTEIN, E. H.: 1-3, diarylindane-2-carboxylic acids, potent and selective non-peptide endothelin receptor antagonists. J. Med. Chem. 37: 1553-1557, 1994.
6. ELSHOURBAGY, N., KORMAN, D., NUTHULAOANTI, P., Wu, H-L., SYLVESTER, D., KUMAR, C., BERGSMA, D. AND NAMBI, P.: Molecular characterization and regulation of the human endothelin receptors. J. Biol. Chem. 268: 3873-3879, 1993.
7. A receptor antagonist in the rat. J. Clin. Invest. 93: 900-906, 1994.
8. GELLAI, M., JUGUS, M., FLETCHER, T. A., NAMBI, P., OHLSTEIN, E. H., ELLIOTT, J. D. AND BROOKS, D. P.: Nonpeptide endothelin receptor antagonists V. Prevention and reversal of acute renal failure in the rat by SB 209670. J. Pharmacol. Exp. Ther. 275: 200-206, 1995.
9. A receptors. Life Sci. 50: 247-255, 1992.
10. INOUE, A., YANAGISAWA, M., KIMURA, S., KASUYA, Y., MIYAUCHI, T., GOTO, K. AND MASAKI, T.: The human endothelial family: Three structurally and pharmacologically distinct isopeptides predicted by three separate genes. Proc. Natl. Acad. Sci. USA 86: 2863-2867, 1989.
11. KLOOG, Y. AND SOKOLOVSKY, M.: Similarities in mode and sites of action of sarafotoxins and endothelins. Trends Pharmacol. Sci. 10: 212-214, 1989.
12. KLOOG, Y., AMBAR, I., SOKOLOVSKY, M. AND WOLLBERG, Z. SARAFOTOXIN, A NOVEL VASOCONSTRICTOR PEPTIDE: phosphoinositide hydrolysis in rat heart and brain. Science (Wash., DC) 242: 268-270, 1988.
13. MARTINS, E. R., BRENNER, B. M. AND BALLERMAN, B. J.: Heterogeneity of cell surface endothelin receptors. J. Biol. Chem. 265: 14044-14049, 1990.
14. NAMBI, P., ELSHOURBAGY, N., WU, H-L., PULLEN, M., OHLSTEIN, E., BROOKS, D. P., LAGO, A., ELLIOTT, J. D., GLEASON, J. AND RUFFOLO, R. R.: Nonpeptide endothelin receptor antagonists I. Effects on binding and signal transduction on human ETA and ETB receptors. J. Pharmacol. Exp. Ther. 271: 755-761, 1994a.
15. NAMBI, P., PULLEN, M. AND FEUERSTEIN, G.: Identification of endothelin receptors in various regions of rat brain. Neuropeptides 18:195-199, 1990.
16. B receptors. J. Pharmacol. Exp. Ther. 268: 202-207, 1994b.
17. NAMBI, P., PULLEN, M., WU, H-L., AIYAR, N., OHLSTEIN, E. H. AND EDWARDS, R. M.: Identification of endothelin receptor subtypes in human renal cortex and medulla using subtype-selective ligands. Endocrinology 131: 1081-1086, 1992a.
18. NAMBI, P., Wu, H-L., PULLEN, M., AIYAR, N., BRYAN, H. AND ELLIOTT, J. D.: Identification of endothelin receptor subtypes in rat kidney cortex using subtype-selective ligands. Mol. Pharmacol. 42: 336-339, 1992b.
19. OHLSTEIN, E. H., DOUGLAS, S. A., EZEKIEL, M. AND GELLAI, M.: Antihypertensive effects of the endothelin receptor antagonist BQ123 in conscious spontaneously hypertensive rats. J. Cardiovasc. Pharmacol. 22(Suppl. 8): S321-S324, 1993.
20. OHLSTEIN, E. H., BECK, G., DOUGLAS, S. A., NAMBI, P., GLEASON, J., RUFFOLO, JR., R. R., FEUERSTEIN, G. AND ELLIOTT, J. D.: Non-peptide endothelin receptor antagoniste II. Pharmacological characterization of SB 209670. J. Pharmacol. Exp. Ther. 271: 762-768, 1994.
21. Roux, S. P., CLOZEL, M., SPRECHER, U., GRAY, G. AND CLOZEL, J. P.: Ro 47-0203, a new endothelin receptor antagonist, reverses chronic vasospasm in experimental subarachnoid hemorrhage. Circulation Suppl. 88:1-170, 1993.
22. SAKURAI, T., YANAGISAWA, M., TAKUWA, Y., MIYAZAKI, M., KIMURA, S., GOTO, K. AND MASAKI, T.: Cloning of a cDNA encoding a non-isopeptide-selective subtype of the endothelin receptor. Nature (Lond.) 348: 732-735, 1990.
23. SIMONSON, M. S. AND DUNN, M. J.: Cellular signalling by peptides of the endothelin gene family. FASEB J. 4: 2989-3000, 1990.
24. 125I] IRL-1620. Biochem. Biophys. Res. Commun. 185: 867-873, 1992.
25. WILLIAMS, D. L., JONES, K. L., PETTIBONE, D. J., Lis, E. V. ANDCLINSCHMIDT, B. V.: Sarafotoxin 6c, an agonist which distinguishes between endothelin receptor subtypes. Biochem. Biophys. Res. Commun. 175: 556-561, 1991.
26. YANAGISAWA, M., KURIHARA, M., KIMURA, S., TOMBE, Y., KOBAYASHI, M., Mrrsui, Y., YAZAKI, Y., GOTO, K. AND MASAKI, T. ENDOTHELIN: A novel potent vasoconstrictor peptide produced by vascular endothelial cells. Nature (Lond.) 332: 411-415, 1988.