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Chemical Compound Review

Tocris-1210     (2R)-2-[[(2R)-2-[[(2S)-2- (azepan-1...

Synonyms: CHEMBL352396, SureCN2124350, CHEBI:385873, LS-16125, DCL000377, ...
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Disease relevance of FR139317


High impact information on FR139317


Chemical compound and disease context of FR139317


Biological context of FR139317

  • This coronary vasoconstriction was substantially reversed by treatment either with antibody against TNF-alpha or with FR 139317 [12].
  • An endothelin type A receptor antagonist, FR139317, negated the inhibitory effect of ET-1 on apoptosis, while the endothelin type B receptor antagonist BQ788 did not show such a negation [13].
  • BQ123 (cyclo[D-Trp-D-Asp-Pro-D-Val-Leu]) and FR139317 (cC6N-L-Leu-D-Trp-Me-D-2Pya-OH), two antagonists that are selective for the ETA receptor, inhibited 125I-ET-1 binding with IC50 values of 5 nM and 0.9 nM, respectively [14].
  • The phosphatidylinositol hydrolysis response was also inhibited by BQ123 and FR139317 [14].
  • In contrast, FR139317 showed low affinity for [125I]ET-1 specific binding sites in porcine kidney (IC50, 4.7 microM) [15].

Anatomical context of FR139317


Associations of FR139317 with other chemical compounds

  • Incubation of arteries from hypercholesterolemic pigs with BQ-788 (ETB-receptor antagonist), but not FR-139317 (ETA-receptor antagonist), altered the contractile response to ET-1 at 10(-10) mol/L [21].
  • L-NAME (0.46 to 7.42 micromol/kg [0.125 to 2 mg/kg]) induced a dose-dependent increase in blood pressure, which was attenuated by 60% and 48% with bosentan and FR 139317, respectively (P<.01) [22].
  • Cyclosporine (25 mg/kg per day) given for 4 weeks increased blood pressure from 98 +/- 12 to 156 +/- 14 mm Hg; this increase was blunted by coadministration of 10 mg/kg per day FR 139317 (ie, blood pressure was 138 +/- 14 mm Hg) in Wistar-Kyoto rats [23].
  • Blood pressure, urinary protein excretion and serum creatinine were evaluated at days 0, 7 (before FR139317 or saline administration), 30, 45 and 60 [24].
  • The ETA receptor-selective antagonists BQ-123 and FR139317 caused concentration-dependent inhibition of the contractions induced by endothelin-1 and sarafotoxin S6b, but both antagonists were significantly less potent in inhibiting contractions induced by endothelin-1 than sarafotoxin S6b [25].

Gene context of FR139317

  • Moreover, the ETB receptor agonist sarafotoxin S6c induced contraction in vessels preincubated with FR139317 [26].
  • In addition, the ET(A)-selective antagonist FR139317 inhibited ET-1-induced leptin expression more potently than did the ET(B)-selective antagonist BQ788 [27].
  • In addition, the effect of the specific endothelin type A receptor antagonist FR 139317 on FK 506-induced hypertension in rats was studied [3].
  • Analysis of the role of endothelin-A and endothelin-B receptors on nociceptive information transmission in the spinal cord with FR139317, an endothelin-A receptor antagonist, and sarafotoxin S6c, an endothelin-B receptor agonist [28].
  • 6. The results show that the ETA antagonists, BQ123 and FR139317, are highly selective for ETA receptors in all cardiac tissues tested, whereas BQ788 has a low affinity and no selectivity in this human tissue [29].

Analytical, diagnostic and therapeutic context of FR139317


  1. Comparison of the effects of selective endothelin ETA and ETB receptor antagonists in congestive heart failure. Wada, A., Tsutamoto, T., Fukai, D., Ohnishi, M., Maeda, K., Hisanaga, T., Maeda, Y., Matsuda, Y., Kinoshita, M. J. Am. Coll. Cardiol. (1997) [Pubmed]
  2. Endogenous endothelin-1 mediates cardiac hypertrophy and switching of myosin heavy chain gene expression in rat ventricular myocardium. Ichikawa, K.I., Hidai, C., Okuda, C., Kimata, S.I., Matsuoka, R., Hosoda, S., Quertermous, T., Kawana, M. J. Am. Coll. Cardiol. (1996) [Pubmed]
  3. Mechanisms of FK 506-induced hypertension in the rat. Takeda, Y., Miyamori, I., Furukawa, K., Inaba, S., Mabuchi, H. Hypertension (1999) [Pubmed]
  4. Role of endothelin as a mitogen in experimental glomerulonephritis in rats. Fukuda, K., Yanagida, T., Okuda, S., Tamaki, K., Ando, T., Fujishima, M. Kidney Int. (1996) [Pubmed]
  5. The role of endothelin-A receptors in cardiovascular responses to acute hypoxaemia in the late gestation sheep fetus. Green, L.R., McGarrigle, H.H., Bennet, L., Hanson, M.A. J. Physiol. (Lond.) (1998) [Pubmed]
  6. Systemic hypertension induced by hepatic overexpression of human preproendothelin-1 in rats. Niranjan, V., Télémaque, S., deWit, D., Gerard, R.D., Yanagisawa, M. J. Clin. Invest. (1996) [Pubmed]
  7. Angiotensin converting enzyme inhibition modulates endogenous endothelin in chronic canine thoracic inferior vena caval constriction. Clavell, A.L., Mattingly, M.T., Stevens, T.L., Nir, A., Wright, S., Aarhus, L.L., Heublein, D.M., Burnett, J.C. J. Clin. Invest. (1996) [Pubmed]
  8. Effects of a specific endothelin-converting enzyme inhibitor on cardiac, renal, and neurohumoral functions in congestive heart failure: comparison of effects with those of endothelin A receptor antagonism. Wada, A., Tsutamoto, T., Ohnishi, M., Sawaki, M., Fukai, D., Maeda, Y., Kinoshita, M. Circulation (1999) [Pubmed]
  9. ETA receptor antagonists inhibit allergic inflammation in the mouse. Sampaio, A.L., Rae, G.A., D'Orléans-Juste, P., Henriques, M.G. J. Cardiovasc. Pharmacol. (1995) [Pubmed]
  10. Effects of the endothelin ETA-receptor antagonist FR139317 on development of hypertension and cardiovascular hypertrophy in deoxycorticosterone acetate-salt hypertensive rats. Fujita, K., Matsumura, Y., Miyazaki, Y., Takaoka, M., Morimoto, S. Jpn. J. Pharmacol. (1996) [Pubmed]
  11. Effects of endothelin receptor A antagonist FR139317 on rats with congestive heart failure. Chen, X.C., Zhang, X.M., Luo, N.S., Fang, C., Liu, Y.M., Wu, W. Acta Pharmacol. Sin. (2001) [Pubmed]
  12. Endothelin 1 mediates ex vivo coronary vasoconstriction caused by exogenous and endogenous cytokines. Klemm, P., Warner, T.D., Hohlfeld, T., Corder, R., Vane, J.R. Proc. Natl. Acad. Sci. U.S.A. (1995) [Pubmed]
  13. Endothelin-1 as a protective factor against beta-adrenergic agonist-induced apoptosis in cardiac myocytes. Araki, M., Hasegawa, K., Iwai-Kanai, E., Fujita, M., Sawamura, T., Kakita, T., Wada, H., Morimoto, T., Sasayama, S. J. Am. Coll. Cardiol. (2000) [Pubmed]
  14. Identification and characterization of type A endothelin receptors in MMQ cells. Wu-Wong, J.R., Chiou, W., Magnuson, S.R., Witte, D.G., Lin, C.W. Mol. Pharmacol. (1993) [Pubmed]
  15. Pharmacological profile of FR139317, a novel, potent endothelin ETA receptor antagonist. Sogabe, K., Nirei, H., Shoubo, M., Nomoto, A., Ao, S., Notsu, Y., Ono, T. J. Pharmacol. Exp. Ther. (1993) [Pubmed]
  16. Endothelin receptor antagonists in a beagle model of pulmonary hypertension: contribution to possible potential therapy? Okada, M., Yamashita, C., Okada, M., Okada, K. J. Am. Coll. Cardiol. (1995) [Pubmed]
  17. ETA and ETB receptors mediate contraction to endothelin-1 in renal artery of aging SHR. Effects of FR139317 and bosentan. Seo, B., Lüscher, T.F. Hypertension (1995) [Pubmed]
  18. Endothelin receptor subtypes in small arteries. Studies with FR139317 and bosentan. Takase, H., Moreau, P., Lüscher, T.F. Hypertension (1995) [Pubmed]
  19. BQ788, an endothelin ET(B) receptor antagonist, attenuates stab wound injury-induced reactive astrocytes in rat brain. Koyama, Y., Takemura, M., Fujiki, K., Ishikawa, N., Shigenaga, Y., Baba, A. Glia (1999) [Pubmed]
  20. The effects of the endothelin ETA receptor antagonist, FR 139317, on infarct size in a rabbit model of acute myocardial ischaemia and reperfusion. McMurdo, L., Thiemermann, C., Vane, J.R. Br. J. Pharmacol. (1994) [Pubmed]
  21. Enhanced endothelin-B-receptor-mediated vasoconstriction of small porcine coronary arteries in diet-induced hypercholesterolemia. Hasdai, D., Mathew, V., Schwartz, R.S., Smith, L.A., Holmes, D.R., Katusic, Z.S., Lerman, A. Arterioscler. Thromb. Vasc. Biol. (1997) [Pubmed]
  22. Endogenous endothelin modulates blood pressure, plasma volume, and albumin escape after systemic nitric oxide blockade. Filep, J.G. Hypertension (1997) [Pubmed]
  23. Effects of an endothelin receptor antagonist in rats with cyclosporine-induced hypertension. Takeda, Y., Miyamori, I., Wu, P., Yoneda, T., Furukawa, K., Takeda, R. Hypertension (1995) [Pubmed]
  24. A specific endothelin subtype A receptor antagonist protects against injury in renal disease progression. Benigni, A., Zoja, C., Corna, D., Orisio, S., Longaretti, L., Bertani, T., Remuzzi, G. Kidney Int. (1993) [Pubmed]
  25. Typical endothelin ETA receptors mediate atypical endothelin-1-induced contractions in sheep isolated tracheal smooth muscle. Henry, P.J., King, S.H. J. Pharmacol. Exp. Ther. (1999) [Pubmed]
  26. Both ETA and ETB receptors mediate contraction to endothelin-1 in human blood vessels. Seo, B., Oemar, B.S., Siebenmann, R., von Segesser, L., Lüscher, T.F. Circulation (1994) [Pubmed]
  27. Endothelin-1 stimulates leptin production in adipocytes. Xiong, Y., Tanaka, H., Richardson, J.A., Williams, S.C., Slaughter, C.A., Nakamura, M., Chen, J.L., Yanagisawa, M. J. Biol. Chem. (2001) [Pubmed]
  28. Analysis of the role of endothelin-A and endothelin-B receptors on nociceptive information transmission in the spinal cord with FR139317, an endothelin-A receptor antagonist, and sarafotoxin S6c, an endothelin-B receptor agonist. Yamamoto, T., Shimoyama, N., Asano, H., Mizuguchi, T. J. Pharmacol. Exp. Ther. (1994) [Pubmed]
  29. Characterization of the endothelin receptor selective agonist, BQ3020 and antagonists BQ123, FR139317, BQ788, 50235, Ro462005 and bosentan in the heart. Peter, M.G., Davenport, A.P. Br. J. Pharmacol. (1996) [Pubmed]
  30. Regional variation in appearance of vascular contractile endothelin-B receptors following organ culture. Adner, M., Uddman, E., Cardell, L.O., Edvinsson, L. Cardiovasc. Res. (1998) [Pubmed]
  31. Evidence from receptor antagonists of an important role for ETB receptor-mediated vasoconstrictor effects of endothelin-1 in the rat kidney. Wellings, R.P., Corder, R., Warner, T.D., Cristol, J.P., Thiemermann, C., Vane, J.R. Br. J. Pharmacol. (1994) [Pubmed]
  32. Renal vascular effects of the selective endothelin receptor antagonists in anaesthetized rats. Matsuura, T., Miura, K., Ebara, T., Yukimura, T., Yamanaka, S., Kim, S., Iwao, H. Br. J. Pharmacol. (1997) [Pubmed]
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