Pharmacological characterization of A-127722: An orally active and highly potent ETA-selective receptor antagonist

Journal of Pharmacology and Experimental Therapeutics

Volumn 276, Issue 2, 1996, Pages 473-481

  Opgenorth, Terry J ^a   Adler, Andrew L ^a   Calzadilla, Samuel V ^a   Chiou, William J ^a   Dayton, Brian D ^a   Dixon, Douglas B ^a   Gehrke, Laura J ^a   Hernandez, Lisa ^a   Magnuson, Scott R ^a   Marsh, Kennan C ^a   Novosad, Eugene I ^a   Von Geldern, Thomas W ^a   Wessale, Jerry L ^a   Winn, Martin ^a   Wu Wong, Jinshyun R ^a  

^a ABBOTT LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ARACHIDONIC ACID; ATRASENTAN; ENDOTHELIN A RECEPTOR; ENDOTHELIN RECEPTOR; PHOSPHATIDYLINOSITOL; PYRROLIDINE DERIVATIVE;

ANIMAL; ARTICLE; CHO CELL; DOG; DRUG ANTAGONISM; DRUG EFFECT; FEMALE; HAMSTER; HUMAN; MACACA; MALE; METABOLISM; ORAL DRUG ADMINISTRATION; RAT; SPRAGUE DAWLEY RAT; STEREOISOMERISM; VASOCONSTRICTION;

ADMINISTRATION, ORAL; ANIMALS; ARACHIDONIC ACID; CHO CELLS; CRICETINAE; DOGS; FEMALE; HUMANS; MACACA FASCICULARIS; MALE; PHOSPHATIDYLINOSITOLS; PYRROLIDINES; RATS; RATS, SPRAGUE-DAWLEY; RECEPTOR, ENDOTHELIN A; RECEPTORS, ENDOTHELIN; STEREOISOMERISM; VASOCONSTRICTION;

EID: 0030077247     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (38)

1. ARAI, H., HORI, S., ARAMORI, I., OHKUBO, H. AND NAKANISHI, S.: Cloning and expression of a cDNA encoding an endothelin receptor. Nature (Lond.) 348: 730-732, 1990.
2. ARAI, H., NAKAO, K., TAKAYA, K., HOSODA, K., OGAWA, Y., NAKANISHI, S. AND IMURA, H.: The human endothelin-B receptor gene. J. Biol. Chem. 268: 3463-3470, 1993.
3. ARAMORI, I., NIREI, H., SHOUBO, M., SOGABE, K., NAKAMURA, K., KOJO, H., NOTSU, Y., ONO, T. AND NAKANISHI, S.: Subtype selectivity of a novel endothelin antagonist, FR139317, for the two endothelin receptors in transfected Chinese hamster ovary cells. Mol. Pharmacol. 43: 127-131, 1993.
4. ARUNLAKSHANA, O. AND SCHILD, H.: Some quantitative uses of drug antagonists. Br. J. Pharmacol. 14: 48-58, 1956.
5. BAX, W. AND SAXENA, P.: The current endothelin receptor classification: Time for reconsideration? Trends Pharmacol. Sci. 15: 379-386, 1994.
6. A receptor antagonist. Eur. J. Pharmacol. 240: 295-298, 1993.
7. CLOZEL, M., BREU, V., BURRI, K., CASSAL, J.-M., FISCHLI, W., GRAY, G. A., HIRTH, G., LOFFLER, B.-M., MULLER, M., NEIDHART, W. AND RAMUZ, H.: Pathophysio-logical role of endothelin revealed by the first orally active endothelin receptor antagonist. Nature (Lond.) 365: 759-761, 1993.
8. CLOZEL, M., BREU, V., GRAY, G., KALINA, B., LOFFLER, B.-M., BURRI, K., CASSAL, J.-M., HIRTH, G., MULLER, M., NEIDHART, W. AND RAMUZ, H.: Pharmacological characterization of bosentan, a new potent orally active nonpeptide endothelin receptor antagonist. J. Pharmacol. Exp. Ther. 270: 228-235, 1994.
9. A receptors in humans? Trends Pharmacol. Sci. 15: 9-11, 1994
10. B mRNA and receptors are expressed by smooth muscle in the human vasculature: Majority of the ETA subtype. Br. J. Pharmacol. 114: 1110-1116, 1995.
11. ELSHOURBAGY, N. A., KORMAN, D. R., WU, H.-L., SYLVESTER, D. R., LEE, J. A., NUTHALAGANTI, P., BERGSMA, D. J., KUMAR, C. S. AND NAMBI, P.: Molecular characterization and regulation of the human endotheun receptors. J. Biol. Chem. 268: 3873-3879, 1993.
12. B receptors in rats. Biochem. Biophys. Res. Commun. 199: 1461-1465, 1994.
13. HOSODA, K., NAKAO, K., ARAI, H., SUGA, S., OGAWA, Y., MUKOYAMA, M., SHIRAKAMI, G., SAITO, Y., NAKANISHI, S. AND IMURA, H.: Cloning and expression of human endothelin-1 receptor cDNA. FEES Lett. 287: 23-26, 1991.
14. A receptor. Life Sci. 50: 247-255, 1991.
15. ISHIKAWA, K., IHARA, M., NOGUCHI, K., MASE, T., MINO, N., SAEKI, T., FUKURODA, T., FUKAMI, T., OZAKI, S., NAGASE, T., NISHIKIBE, M. AND YANO, M.: Biochemical and pharmacological profile of a potent and selective endothelin B-receptor antagonist, BQ-788. Proc. Natl. Acad. Sci. U.S.A. 91: 4892-4896, 1994.
16. A receptor-induced constrictor responses to endothelin peptides in human blood vessels in vitro. Br. J. Pharmacol. 115: 191-187, 1995.
17. B receptor. Br. J. Pharmacol. 109: 530-534, 1993.
18. MORELAND, S., MCMULLEN, D., ABBOA-OFFEI, B AND SEYMOUR, A.: Evidence for a differential location of vasoconstrictor endothelin receptors in the vasculature. Br J. Pharmacol. 112: 704-708, 1994.
19. OHLSTEIN, E., BECK, G., JR., DOUGLAS, S., NAMBI, P., LAGO, M., GLEASON, J., RUFFLO, R., JR., FEUERSTEIN, G. AND ELLIOT, J.: Nonpeptide endothelin receptor antagonists. II. Pharmacological characterization of SB 209670. J. Pharmacol. Exp. Ther. 271: 762-768, 1994a
20. OHLSTEIN, E., NAMBI, P., DOUGLAS, S., EDWARDS, R., GELLAI, M., LAGO, A., LEBER, J., COUSINS, R., GAO, A., FRAZEE, J., PEISHOFF, C., BEAN, J., EGGLESTON, D. S., ELSHOURBAGY, N., KUMAR, C., LEE, J., YUE, T.-L., LOUDEN, C., BROOKS, D., WEINSTOCK, J., FEUERSTEIN, G., POSTE, G., RUFFOLO, R., JR., GLEASON, J. AND ELLIOT, J.: SB 209670, a rationally designed potent nonpeptide endothelin receptor antagonist. Proc. Natl. Acad. Sci. U.S.A. 91: 8052-8056, 1994b.
21. OPGENORTH, T.: Endothelin receptor antagonism. Adv. Pharmacol. 33: 1-65, 1995.
22. PANEK, R., MAJOR, T., HINGORANI, G., DOHERTY, A., TAYLOR, D. AND RAPUNDALO, S.: Endothelin and structurally related analogs distinguish between, endothelin receptor subtypes. Biochem. Biophys. Res. Commun. 183: 566-571, 1992.
23. A receptor activation. Am. J. Physiol. 264: R222-R226, 1993.
24. A receptor antagonist. J. Pharmacol Exp. Ther. 273: 1410-1417, 1995.
25. RUBANYI, G. AND POLOKOFF, M.: Endothelins: Molecular biology, biochemistry, pharmacology, physiology, and pathophysiology. Pharmacol. Rev. 46: 325-415, 1994.
26. SAKURAI, T., YANAGISAWA, M., TAKUWA, Y., MIYAZAKI, H., KIMURA, S., GOTO, K. AND MASAKI, T.: Cloning of a cDNA encoding a non-isopeptide-selective subytpe of the endothelin receptor. Nature (Lond.) 348: 732-735, 1990.
27. SEDMAN, A. AND WAGNER, J.: CSTRIP-A FORTRAN computer program for obtaining initial polyexponential estimates. J. Pharm. Sci. 65: 1006-1010, 1976.
28. B receptors mediate contraction to endothelin-1 in human blood vessels. Circulation 89: 1203-1208, 1994.
29. SIMONSON, M. S.: Endothelins: Multifunctional renal peptides. Physiol. Rev. 73: 375-411, 1993.
30. A receptor antagonist. J. Pharmacol. Exp. Ther. 264: 1040-1046, 1993.
31. STATISTICAL CONSULTANTS, I.: PCNONLIN and NONLIN84: Software for the statistical analysis of nonlinear models. Am. Stat. 40: 52, 1986.
32. WARNER, T. D., MITCHELL, J. A., DE NUCCI, G. AND VANE, J. R.: Endothelin-1 and endothelin-3 release EDRF from isolated perfused arterial vessels of the rat and rabbit. J. Cardiovasc. Pharmacol. 13: suppl. 5, S85-S88, 1989.
33. A receptor antagonist. J. Pharmcol. Exp. Ther. 272: 1124-1134, 1995.
34. A selective endothelin receptor antagonists (I) Structure activity relationships of the N-substituent. J. Med. Chem., in press.
35. WU-WONG, J. R., CHIOU, W., HUANG, Z.-J., VIDAL, M. AND OPGENORTH, T. J.: Endothelin receptors in human smooth muscle cells: Antagonist potency differs on agonist-evoked responses. Am. J. Physiol. 267: C1185-C1195, 1994a.
36. WU-WONG, J. R., CHIOU, W. J., MAGNUSON, S. R. AND OPGENORTH, T. J.: Endothelin receptor agonists and antagonists exhibit different dissociation characteristics. Biochim. Biophys. Acta 1224: 288-294, 1994b.
37. WU-WONG, J. R , CHIOU, W., MAGNUSON, S , WITTE, D. AND LIN, C.: Identification and characterization of Type-A endothelin receptors in MMQ cells. Mol. Pharmacol. 44: 285-291, 1993.
38. YANAGISAWA, M., KURIHAKA, H., KIMURA, S., TOMOBE, Y., KOBAYASHI, M., MITSUI, Y., YAZAKI, Y., GOTO, K. AND MASAKI, T.: A novel potent vasoconstrictor peptide produced by vascular endothelial cells. Nature (Lond.) 332: 411-414, 1988.