Pharmacological profile of T-0201, a highly potent and orally active endothelin receptor antagonist

Journal of Pharmacology and Experimental Therapeutics

Volumn 286, Issue 2, 1998, Pages 643-649

  Hoshino, Tomoko ^a   Yamauchi, Rikako ^a   Kikkawa, Kohei ^a   Yabana, Hideo ^a   Murata, Sakae ^a  

^a MITSUBISHI TANABE PHARMA CORPORATION   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

ENDOTHELIN 1; ENDOTHELIN A RECEPTOR; ENDOTHELIN A RECEPTOR ANTAGONIST; ENDOTHELIN B RECEPTOR; N [6 [2 (5 BROMOPYRIMIDIN 4 YL)] 4 (2 HYDROXY 1,1 DIMETHYLETHYL)]BENZENSULFONAMIDE SODIUM SESQUIHYDRATE; SARAFOTOXIN S6C; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BLOOD VESSEL REACTIVITY; CHO CELL; CONTROLLED STUDY; DOSE RESPONSE; DRUG MECHANISM; DRUG POTENCY; DRUG RECEPTOR BINDING; INTRAVENOUS DRUG ADMINISTRATION; MALE; NONHUMAN; ORAL DRUG ADMINISTRATION; PRIORITY JOURNAL; RAT; SMOOTH MUSCLE CONTRACTION;

ANIMALS; BLOOD PRESSURE; CELL MEMBRANE; CHO CELLS; CLONING, MOLECULAR; CRICETINAE; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; IODINE RADIOISOTOPES; MALE; MUSCLE CONTRACTION; MUSCLE, SMOOTH, VASCULAR; POTASSIUM CHLORIDE; PYRIMIDINES; RABBITS; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, ENDOTHELIN; SULFONAMIDES;

EID: 0032424117     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (31)

1. Arai H, Hori S, Aramori I, Ohkubo H and Nakanishi S (1990) Cloning and expression of a cDNA encoding an endothelin receptor. Nature (Lond). 348:730-732.
2. Arunlakshana O and Schild H (1956) Some quantitative uses of drug antagonists. Br J Pharmacol 14:48-58.
3. Battistini B, Chailler P, D'orléans-Juste P, Briére N and Sirois P (1993) Growth regulatory properties of endothelins. Peptides 14:385-399.
4. Chen S-J, Chen Y-F, Meng QC, Durand J, Dicarlo VS and Oparil S (1995) Endothelin-receptor antagonist bosentan prevents and reverses hypoxic pulmonary hypertension in rats. J Appl Physiol 79:2122-2131.
5. 50) of an enzymatic reaction. Biochem Pharmacol 22:3099-3109.
6. Clozel M, Breu V, Burri K, Cassai J-M, Fischli W, Gray GA, Hirth G, Löffler BM, Müller M, Neidhart W and Ramuz H (1993) Pathophysiological role of endothelin revealed by the first orally active endothelin receptor antagonist. Nature (Lond.) 365:759-761.
7. Clozel M, Breu V, Gray GA, Kalina B, Löffler B-M, Burri K, Cassal J-M, Hirth G, Müller M, Neidhart W and Ramuz H (1994) Pharmacological characterization of bosentan, a new potent orally active nonpeptide endothelin receptor antagonist. J Pharmacol Exp Ther 270:228-235.
8. Clozel M, Fischli W and Guilly C (1989) Specific binding of endothelin on human vascular smooth muscle cells in culture. J Clin Invest 83:1758-1761.
9. De Nucci G, Thomas R, D'Orleans-Juste P, Antunes E, Walder C, Warner TD and Vane JR (1988) Pressor effects of circulating endothelin are limited by its removal in the pulmonary circulation and by release of prostacyclin and endothelium-derived relaxing factor. Proc Natl Acad Sci USA 85:9797-9800.
10. Eddahibi S, Raffestin B, Clozel M, Levame M and Adnot S (1995) Protection from pulmonary hypertension with an orally active endothelin receptor antagonist in hypoxic rats. Am J Physiol 268:H828-H835.
11. Fukuroda T, Ozaki S, Ihara M, Ishikawa K, Yano M and Nishikibe M (1994) Synergistic inhibition by BQ-123 and BQ-788 of endothelin-1-induced contractions of the rabbit pulmonary artery. Br J Pharmacol 113:336-338.
12. Haleen SJ, Davis LS, LaDouceur DM and Keiser JA (1993) Why big endothelin-1 lacks a vasodilator response. J Cardiovasc Pharmacol 22:suppl. 8, S271-S273.
13. B receptors and multiple signal transduction systems. Br J Pharmacol 110:435-441.
14. Inoue A, Yanagisawa M, Kimura S, Kasuya Y, Miyauchi T, Goto K and Masaki T (1989) The human endothelin family: Three structurally and pharmacologically distinct isopeptides predicted by three separate genes. Proc Natl Acad Sci USA 86:2863-2867.
15. B receptor antagonist. Circulation 93:2068-2079.
16. B receptors coexist on rabbit pulmonary artery vascular smooth muscle mediating contraction. Biochem Biophys Res Commun 196:209-215.
17. Li JS, Larivière R and Schiffrin EL (1994) Effect of a nonselective endothelin antagonist on vascular remodeling in deoxycorticosterone acetate-salt hypertensive rats: Evidence for a role of endothelin in vascular hypertrophy. Hypertension 24:183-188.
18. Lin HY, Kaji EH, Winkel GK, Ives HE and Lodish HF (1991) Cloning and functional expression of a vascular smooth muscle endothelin 1 receptor. Proc Natl Acad Sci USA 88:3185-3189.
19. Mihara S and Fujimoto M (1991) Non-isopeptide-selective endothelin receptors in human girardi heart cells. Life Sci 50:219-226.
20. Miller RC, Pelton JT and Huggins JP (1993) Endothelins - from receptors to medicine. Trends Pharmacol Sci 14:54-60.
21. Mulder P, Richard V, Derumeaux G, Hogie M, Henry JP, Lallemand F, Compagnon P, Macé B, Comoy E, Letac B and Thuillez C (1997) Role of endogenous endothelin in chronic heart failure: Effect of long-term treatment with an endothelin antagonist on survival, hemodynamics, and cardiac remodeling. Circulation 96:1976-1982.
22. Ohlstein EH, Nambi P, Douglas SA, Edwards RM, Gellai M, Lago A, Leber JD, Cousins RD, Gao A, Frazee JS, Peishoff CE, Bean JW, Eggleston DS, Elshourbagy NA, Kumar C, Lee JA, Yue T-L, Louden C, Brooks DP, Weinstock J, Feuerstein G, Poste G, Ruffolo RR Jr, Gleason JG and Elliott JD (1994) SB 209670, a rationally designed potent nonpeptide endothelin receptor antagonist. Proc Natl Acad Sci USA 91:8052-8056.
23. Panek RL, Major TC, Hingorani GP, Doherty AM, Taylor DG and Rapundalo ST (1992) Endothelin and structurally related analogs distinguish between endothelin receptor subtypes. Biochem Biophys Res Commun 183:566-571.
24. Rubanyi GM and Polokoff MA (1994) Endothelins: Molecular biology, biochemistry, pharmacology, physiology, and pathophysiology. Pharmacol Rev 46:328-415.
25. Sakurai T, Yanagisawa M, Takuwa Y, Miyazaki H, Kimura S, Goto K and Masaki T (1990) Cloning of a cDNA encoding a non-isopeptide-selective subtype of the endothelin receptor. Nature (Lond.) 348:732-735.
26. Scatchard G (1949) The attractions of proteins for small molecules and ions. Ann N Y Acad Sci 51:660-670.
27. Shimoyama H, Sabbah HN, Borzak S, Tanimura M, Shevlyagin S, Scicli G and Goldstein S (1996) Short-term hemodynamic effect of endothelin receptor blockade in dogs with chronic heart failure. Circulation 94:779-784.
28. Takayanagi R, Kitazumi K, Takasaki C, Ohnaka K, Aimoto S, Tasaka K, Ohashi M and Nawata H (1991) Presence of non-selective type of endothelin receptor on vascular endothelium and its linkage to vasodilation. FEBS Lett 282:103-106.
29. Wang Q-D, Li X-S, Lundberg JM and Pernow J (1995) Protective effects of non-peptide endothelin receptor antagonist bosentan on myocardial ischemic and reperfusion injury in the pig. Cardiovasc Res 29:805-812.
30. Yanagisawa M, Inoue A, Ishikawa T, Kasuya Y, Kimura S, Kumagaye S, Nakajima K, Watanabe TX, Sakakibara S, Goto K and Masaki T (1988b) Primary structure, synthesis, and biological activity of rat endothelin, an endothelium-derived vasoconstrictor peptide. Proc Natl Acad Sci USA 85:6964-6967.
31. Yanagisawa M, Kurihara H, Kimura S, Tomobe Y, Kobayashi M, Mitui Y, Yazaki Y, Goto K and Masaki T (1988a) A novel potent vasoconstrictor peptide produced by vascular endothelial cells. Nature (Lond.) 332:411-415.