Pharmacokinetics and pharmacodynamics of SB 209670, an endothelin receptor antagonist: Effects on the regulation of renal vascular tone

Clinical Pharmacology and Therapeutics

Volumn 65, Issue 5, 1999, Pages 473-482

  Freed, Martin I ^a   Wilson, Douglas E ^b   Thompson, Kathleen A ^b   Harris, Robert Z ^b   Ilson, Bernard E ^b   Jorkasky, Diane K ^b  

^a Clinical Research   (United States)

^b NONE

Author keywords

[No Author keywords available]

Indexed keywords

3 (2 CARBOXYMETHOXY 4 METHOXYPHENYL) 1 (3,4 METHYLENEDIOXYPHENYL) 5 PROPOXY 2 INDANCARBOXYLIC ACID; ENDOTHELIN RECEPTOR ANTAGONIST;

ARTICLE; BLOOD VESSEL REACTIVITY; BLOOD VESSEL TONE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DRUG EFFECT; DRUG SAFETY; HUMAN; KIDNEY BLOOD FLOW; MALE; NORMAL HUMAN; PRIORITY JOURNAL; SINGLE BLIND PROCEDURE;

ADULT; CROSS-OVER STUDIES; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG ADMINISTRATION SCHEDULE; ENDOTHELIN-1; HUMANS; INDANS; INFUSIONS, INTRAVENOUS; MALE; MIDDLE AGED; RECEPTORS, ENDOTHELIN; REFERENCE VALUES; RENAL CIRCULATION; RENAL PLASMA FLOW, EFFECTIVE; SINGLE-BLIND METHOD; VASCULAR RESISTANCE;

EID: 0032915594     PISSN: 00099236     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0009-9236(99)70066-4     Document Type: Article

References (34)

1. 1. Yanagisawa M, Kurihara H, Kimura S, Tomobe Y, Kobayashi M, Mitsui Y, et al. Endothelin: a novel potent vasoconstrictor peptide produced by vascular endothelial cells. Nature 1988;332:411-5.
2. 2. Haynes WG, Webb DJ. The endothelin family of peptides: local hormones with diverse roles in health and disease? Clin Sci 1993;84:485-500.
3. 3. Brain SD, Crossman DC, Buckley TL, Williams TJ. Endothelin-1: demonstration of potent effects on the microcirculation of humans and other species. J Cardiovasc Pharmacol 1989;13(suppl 5):S147-9.
4. 4. Cocks TM, Faulkner NL, Sudhir K, Angus J. Reactivity of endothelin-1 on human and canine large veins compared with large arteries in vitro. Eur J Pharmacol 1989;171:17-24.
5. 2-adrenoceptor- and (endothelium-dependent) neuropeptide Y-mediated contractions in the isolated vascular bed of the rat tail. Br J Pharmacol 1990; 101:205-11.
6. 6. Nakayama K, Ishigai Y, Uchida H, Tanaka Y. Potentiation by endothelin-1 of 5-hydroxytryptamine-induced contraction in coronary artery of the pig. Br J Pharmacol 1991; 104:978-86.
7. 7. Arai H, Hori S, Aramori I, Ohkubo H, Nakanishi S. Cloning and expression of a cDNA encoding an endothelin receptor. Nature 1990;348:730-2.
8. 8. Sakurai T, Yanagisawa M, Yakuwa Y, Miyazaki H, Kimura S, Goto K, et al. Cloning of a cDNA encoding a nonisopeptide selective subtype of the endothelin receptor. Nature 1990;348:732-5.
9. 9. Cristol JP, Warner TD, Thiemerman C, Vane JR. Mediation by different receptors of the vasoconstrictor effects of endothelins and sarafotoxins in the systemic circulation and renal vasculature of the anaesthetized rat. Br J Pharmacol 1993;108:776-9.
10. 10. Panek RL, Major TC, Hingorani GP, Doherty AM, Taylor DG, Rapundalo ST. Endothelin and structurally related analogs distinguish between endothelin receptor subtypes. Biochem Biophys Res Commun 1992;183:566-71.
11. 11. Ohlstein EH, Arleth A, Bryan H, Elliott JD, Sung CP. The selective ETA receptor antagonist BQ-123 antagonizes endothelin-1-mediated mitogenesis. Eur J Pharmacol 1992;225:347-50.
12. 12. Masaki T, Kimura S, Yanagisawa M, Goto K. Molecular and cellular mechanisms of endothelin regulation: implication for vascular function. Circulation 1991;84:1457-68.
13. 13. DeNucci G, Thomas R, D'Orleans-Juste P, Antunes E, Walder C, Warner TD, et al. Pressor effects of circulating endothelin are limited by its removal from the pulmonary circulation and by the release of prostacyclin and endothelium-derived relaxing factor. Proc Natl Acad Sci USA 1988;85:9797-800.
14. 14. Douglas SA, Hiley CR. Endothelium-dependent mesenteric vasorelaxant effects and systemic actions of endothelin (16-21) and other endothelin-related peptides in the rat. Br J Pharmacol 1991;104:311-20.
15. 15. Kohan DE. Endothelins in the kidney: physiology and pathophysiology. Am J Kidney Dis 1993;22:493-510.
16. 16. Rabelink TJ, Kaasjager KAH, Boer P, Stroes EG, Braam B, Koomans HA. Effects of endothelin-1 on renal function in humans: implications for physiology and pathophysiology. Kidney Int 1994;46:376-81.
17. 17. Sørensen SS, Madsen JK, Pedersen EB. Systemic and renal effect of intravenous infusion of endothelin-1 in healthy human volunteers. Am J Physiol 1994;266:F411-8.
18. 18. Ohlstein EH, Nambi P, Douglas SA, Edwards RM, Gellai M, Lago A, et al. SB 209670, a rationally designed potent nonpeptide endothelin receptot antagonist. Proc Natl Sci USA 1994;91:8052-6.
19. 19. Earle DP, Berliner RW. A simplified clinical procedure for measurement of glomerular filtration rate and renal plasma flow. Proc Soc Exp Biol Med 1946;62:262-4.
20. 20. Bratton AC, Marshall EK. A new coupling component for sulfanilamide determination. J Biol Chem 1939;128:537-50.
21. 21. Ramey K, Lee K, Patel V, Selvaggio A, Jorkasky D. Application of p-aminohippuric acid method to the Cobas Mira. Clin Chem 1991;37:982-3.
22. 22. Allen, GD. MODFIT: a pharmacokinetic computer program, Biopharm Drug Dispos 1990;11:477-98.
23. 23. Weber C, Schmitt R, Birnboeck H, Hopfgartner G, van Marle SP, Peeters PA, et al. Pharmacokinetics and pharmacodynamics of the endothelin-receptor antagonist bosentan in healthy human subjects. Clin Pharmacol Ther 1996;60:124-37.
24. 24. Krum H, Viskoper RJ, Lacourciere Y, Budde M, Charlon V. The effect of an endothelin antagonist, bosentan, on blood pressure in patients with essential hypertension. N Engl J Med 1998;338:784-90.
25. 25. Gardiner SM, March JE, Kemp PA, Mullins JJ, Bennett T. Haemodynamic effects of losartan and the endothelin antagonist, SB 209670, in conscious, transgenic ((mRen-2)27), hypertensive rats. Br J Pharmacol 1995;116:2237-44.
26. 26. Teerlink JR, Carteaux JP, Sprecher U, Loffler BM, Clozel M, Clozel JP. Role of endogenous endothelin in normal hemodynamic status of anesthetized dogs. Am J Physiol 1995;269:R469-73.
27. 27. Qui C, Samsell L, Baylis C. Actions of endogenous endothelin in normal on glomerular hemodynamics in the rat. Am J Physiol 1995;269:R469-73.
28. 1-receptor antagonist, in salt-replete healthy men. Clin Pharmacol Ther 1998;63:471-81.
29. A receptor antagonist in the rat. J Clin Invest 1994;93:900-6.
30. 30. Harris PJ, Zhuo J, Mendelsohn FAO, Skinner SL. Haemodynamic and renal tubular effects of low doses of ET in anaesthetized rats. J Physiol 1991;433:25-39.
31. - transporters in rabbit renal cortex. Kidney Int 1992;42:18-24.
32. + exchange. Am J Physiol 1994;266:F658-66.
33. 33. Cody RJ, Haas GJ, Binkley PF, Capers Q, Kelley R. Plasma endothelin correlates with the extent of pulmonary hypertension in patients with chronic congestive heart failure, Circulation 1992;85:504-9.
34. 34. Saito Y, Kazuwa N, Shirakami G, Mukoyama M, Arai H, Hosoda K, et al. Endothelin in patients with chronic renal failure. J Cardiovasc Pharmacol 1991;17:S437-9.