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Chemical Compound Review

BQ-123     2-[(3R,6R,9S,12R,15S)-6-(1H- indol-3...

Synonyms: SureCN1290617, CHEBI:238806, BQ123, AC1L9EDH, C11587, ...
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Disease relevance of BQ 123


High impact information on BQ 123


Chemical compound and disease context of BQ 123


Biological context of BQ 123


Anatomical context of BQ 123

  • Brief intrapulmonary infusions of BQ 123 (0.1-1.0 mcg/min for 10 min) caused sustained increases in left pulmonary artery flow (Qp) without changing main pulmonary artery (MPA) and aortic (Ao) pressures [14].
  • Addition of superoxide dismutase plus catalase or an antagonist of endothelin-A receptors (BQ-123) reduced contractions in rings with endothelium but not in those without endothelium to suspensions of mononuclear cells from rejecting allotransplanted dogs [16].
  • Brachial artery infusion of BQ-123 caused significant forearm vasodilatation in both studies [17].
  • The present study, in human forearm resistance vessels in vivo, was designed to further investigate the physiological function of ET(A) and ET(B) receptor subtypes in human blood vessels and determine the mechanism underlying the vasodilatation to the ET(A)-selective receptor antagonist BQ-123 [17].
  • To characterize the ET receptors present in dog coronary arteries, competition binding assays with radiolabeled ET-1 using ET-1, ET-3, ETA receptor antagonist BQ-123, and sarafotoxin S6c were performed [18].

Associations of BQ 123 with other chemical compounds

  • We examined the contribution of endogenously generated endothelin-1 to maintenance of peripheral vascular tone in healthy subjects by local intraarterial administration of an inhibitor of endothelin converting enzyme, phosphoramidon, and of a selective endothelin receptor A antagonist, BQ-123 [19].
  • METHODS AND RESULTS: In endothelium-denuded IMA and PCA and less so in IMV, FR139317 and BQ-123 (in PCA only) shifted the concentration-contraction curves to ET-1 parallel to the right [20].
  • Interestingly, the positive inotropic effect was completely blocked by selectively damaging endocardial endothelium (Triton X-100, 0.5%, 1-s immersion, n = 7) before ROS generation and by preincubating the muscles with the endothelin-A receptor antagonist BQ 123 (n = 11) [21].
  • CsA elevated blood pressure 17 to 20% in all three groups; renal resistance maximally increased 23, 20, and 23% in vehicle, BQ-123, and BQ-123 and PD 142893 pretreated groups, respectively [22].
  • In one study, six subjects received placebo, the ETA receptor antagonist BQ-123 alone, and BQ-123 in combination with the ETB receptor antagonist BQ-788 after pretreatment with the ACE inhibitor enalapril (E) or placebo [23].

Gene context of BQ 123

  • The specificity of the cardiovascular response to endothelin was demonstrated by the inhibitory effects of the receptor antagonist BQ-123 [24].
  • BQ 123, a selective ETAR antagonist, blocked the ET-1-induced Cx43 phosphorylation and cellular uncoupling [25].
  • METHODS: Forearm blood flow (FBF) responses (strain-gauge plethysmography) to intra-arterial infusion of a selective blocker of ETA receptors (BQ-123) and, on a separate occasion, to ET-1 were measured in 12 hypercholesterolemic patients and 12 normal control subjects [26].
  • BQ-123, an ETA blocker, completely blocked the responsiveness of the MAP kinase to either ET-1 or ET-3 [27].
  • In addition, on a different day, six hypercholesterolemic patients received co-infusion of BQ- 123 and BQ-788 (a selective blocker of ETB receptors) [26].

Analytical, diagnostic and therapeutic context of BQ 123

  • BQ-123, administered just before reperfusion, reduced mucosal damage in the postreperfusion period dose-dependently and improved mean gastric mucosal blood flow and mucosal hemoglobin oxygen saturation during the 30-minute postreperfusion period [28].
  • ET-1 increased the perfusion pressure of collaterals and its effect was significantly suppressed by BQ-123 alone and BQ-123 plus BQ-788, but not BQ-788 alone (P <.05) [29].
  • Bilateral forearm blood flow (FBF) was measured at baseline and following unilateral, subsystemic, intrabrachial artery infusions of ET-1 (2 and 6 pmol/min); BQ-123, a selective ET(A) receptor antagonist (3 and 10 nmol/min); and BQ-788, a selective ET(B) receptor antagonist (0.3 and 1 nmol/min) using venous occlusion plethysmography [30].
  • RESULTS: Intra-arterial infusion of ET-1 significantly increased iliac PWV by 12 +/- 5% (mean +/- STD; p < 0.001), whereas infusion of the endothelin-A (ET(A)) receptor antagonist BQ-123 significantly reduced PWV by 12 +/- 4% (p < 0.001) [31].
  • After 6 weeks of untreated diabetes, rats were implanted with osmotic minipumps which continuously delivered the endothelin-1 antagonist, BQ-123, to the circulation via a jugular vein cannula [32].


  1. Expression and localization of endothelin-1 and endothelin receptors in human meningiomas. Evidence for a role in tumoral growth. Pagotto, U., Arzberger, T., Hopfner, U., Sauer, J., Renner, U., Newton, C.J., Lange, M., Uhl, E., Weindl, A., Stalla, G.K. J. Clin. Invest. (1995) [Pubmed]
  2. Contribution of endogenous endothelin-1 to the progression of cardiopulmonary alterations in rats with monocrotaline-induced pulmonary hypertension. Miyauchi, T., Yorikane, R., Sakai, S., Sakurai, T., Okada, M., Nishikibe, M., Yano, M., Yamaguchi, I., Sugishita, Y., Goto, K. Circ. Res. (1993) [Pubmed]
  3. Endothelin-1 modulates insulin signaling through phosphatidylinositol 3-kinase pathway in vascular smooth muscle cells. Jiang, Z.Y., Zhou, Q.L., Chatterjee, A., Feener, E.P., Myers, M.G., White, M.F., King, G.L. Diabetes (1999) [Pubmed]
  4. Enhanced vasodilatation to endothelin antagonism in patients with compensated cirrhosis and the role of nitric oxide. Helmy, A., Newby, D.E., Jalan, R., Hayes, P.C., Webb, D.J. Gut (2003) [Pubmed]
  5. Effect of BQ-123 and tissue plasminogen activator on vasospasm after subarachnoid hemorrhage in monkeys. Kim, C.J., Bassiouny, M., Macdonald, R.L., Weir, B., Johns, L.M. Stroke (1996) [Pubmed]
  6. Prolonged endothelin A receptor blockade attenuates chronic pulmonary hypertension in the ovine fetus. Ivy, D.D., Parker, T.A., Ziegler, J.W., Galan, H.L., Kinsella, J.P., Tuder, R.M., Abman, S.H. J. Clin. Invest. (1997) [Pubmed]
  7. Growth inhibitory properties of endothelin-1 in human hepatic myofibroblastic Ito cells. An endothelin B receptor-mediated pathway. Mallat, A., Fouassier, L., Préaux, A.M., Gal, C.S., Raufaste, D., Rosenbaum, J., Dhumeaux, D., Jouneaux, C., Mavier, P., Lotersztajn, S. J. Clin. Invest. (1995) [Pubmed]
  8. Prostaglandin E2 abrogates endothelin-induced vasoconstriction in renal outer medullary descending vasa recta of the rat. Silldorff, E.P., Yang, S., Pallone, T.L. J. Clin. Invest. (1995) [Pubmed]
  9. Interaction between endothelial heme oxygenase-2 and endothelin-1 in altered aortic reactivity after hypoxia in rats. Govindaraju, V., Teoh, H., Hamid, Q., Cernacek, P., Ward, M.E. Am. J. Physiol. Heart Circ. Physiol. (2005) [Pubmed]
  10. Nociceptive reaction and thermal hyperalgesia induced by local ET-1 in mice: a behavioral and Fos study. Menéndez, L., Lastra, A., Hidalgo, A., Baamonde, A. Naunyn Schmiedebergs Arch. Pharmacol. (2003) [Pubmed]
  11. Prospective, randomized, double-blind trial of BQ-123 and bosentan for prevention of vasospasm following subarachnoid hemorrhage in monkeys. Hino, A., Weir, B.K., Macdonald, R.L., Thisted, R.A., Kim, C.J., Johns, L.M. J. Neurosurg. (1995) [Pubmed]
  12. Hyperglycemia exaggerates ischemia-reperfusion-induced cardiomyocyte injury: reversal with endothelin antagonism. Verma, S., Maitland, A., Weisel, R.D., Li, S.H., Fedak, P.W., Pomroy, N.C., Mickle, D.A., Li, R.K., Ko, L., Rao, V. J. Thorac. Cardiovasc. Surg. (2002) [Pubmed]
  13. Blunted vascular response to endothelin-a receptor blockade in cyclosporine-treated lung transplant recipients. Silverborn, M., Ambring, A., Nilsson, F., Friberg, P., Jeppsson, A. J. Heart Lung Transplant. (2005) [Pubmed]
  14. Physiologic characterization of endothelin A and B receptor activity in the ovine fetal pulmonary circulation. Ivy, D.D., Kinsella, J.P., Abman, S.H. J. Clin. Invest. (1994) [Pubmed]
  15. Regulation of guinea pig intestinal peristalsis by endogenous endothelin acting at ET(B) receptors. Shahbazian, A., Holzer, P. Gastroenterology (2000) [Pubmed]
  16. Mononuclear cells from dogs with acute lung allograft rejection cause contraction of pulmonary arteries. Cale, A.R., Ricagna, F., Wiklund, L., McGregor, C.G., Miller, V.M. Circulation (1994) [Pubmed]
  17. Endothelin-A receptor antagonist-mediated vasodilatation is attenuated by inhibition of nitric oxide synthesis and by endothelin-B receptor blockade. Verhaar, M.C., Strachan, F.E., Newby, D.E., Cruden, N.L., Koomans, H.A., Rabelink, T.J., Webb, D.J. Circulation (1998) [Pubmed]
  18. Potent vasoconstriction mediated by endothelin ETB receptors in canine coronary arteries. Teerlink, J.R., Breu, V., Sprecher, U., Clozel, M., Clozel, J.P. Circ. Res. (1994) [Pubmed]
  19. Contribution of endogenous generation of endothelin-1 to basal vascular tone. Haynes, W.G., Webb, D.J. Lancet (1994) [Pubmed]
  20. 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]
  21. Endothelin-mediated positive inotropic effect induced by reactive oxygen species in isolated cardiac muscle. De Keulenaer, G.W., Andries, L.J., Sys, S.U., Brutsaert, D.L. Circ. Res. (1995) [Pubmed]
  22. Effects of selective endothelin antagonists on the hemodynamic response to cyclosporin A. Davis, L.S., Haleen, S.J., Doherty, A.M., Cody, W.L., Keiser, J.A. J. Am. Soc. Nephrol. (1994) [Pubmed]
  23. Endothelin A receptor antagonism and angiotensin-converting enzyme inhibition are synergistic via an endothelin B receptor-mediated and nitric oxide-dependent mechanism. Goddard, J., Eckhart, C., Johnston, N.R., Cumming, A.D., Rankin, A.J., Webb, D.J. J. Am. Soc. Nephrol. (2004) [Pubmed]
  24. Endothelin as a neuropeptide. Cardiovascular effects in the brainstem of normotensive rats. Mosqueda-Garcia, R., Inagami, T., Appalsamy, M., Sugiura, M., Robertson, R.M. Circ. Res. (1993) [Pubmed]
  25. Endothelin-1 decreases gap junctional intercellular communication by inducing phosphorylation of connexin 43 in human ovarian carcinoma cells. Spinella, F., Rosanò, L., Di Castro, V., Nicotra, M.R., Natali, P.G., Bagnato, A. J. Biol. Chem. (2003) [Pubmed]
  26. Increased activity of endogenous endothelin in patients with hypercholesterolemia. Cardillo, C., Kilcoyne, C.M., Cannon, R.O., Panza, J.A. J. Am. Coll. Cardiol. (2000) [Pubmed]
  27. Endothelin stimulates mitogen-activated protein kinase activity in mesangial cells through ETA. Wang, Y., Pouysségur, J., Dunn, M.J. J. Am. Soc. Nephrol. (1994) [Pubmed]
  28. Role of endothelin 1 in hemorrhagic shock-induced gastric mucosal injury in rats. Michida, T., Kawano, S., Masuda, E., Kobayashi, I., Nishimura, Y., Tsujii, M., Hayashi, N., Takei, Y., Tsuji, S., Nagano, K. Gastroenterology (1994) [Pubmed]
  29. Endothelin-1 induces vasoconstriction on portal-systemic collaterals of portal hypertensive rats. Chan, C.C., Wang, S.S., Lee, F.Y., Chang, F.Y., Lin, H.C., Chu, C.J., Chen, C.T., Huang, H.C., Lee, S.D. Hepatology (2001) [Pubmed]
  30. Altered peripheral vascular responses to exogenous and endogenous endothelin-1 in patients with well-compensated cirrhosis. Helmy, A., Jalan, R., Newby, D.E., Johnston, N.R., Hayes, P.C., Webb, D.J. Hepatology (2001) [Pubmed]
  31. Endothelin-1 regulates arterial pulse wave velocity in vivo. McEniery, C.M., Qasem, A., Schmitt, M., Avolio, A.P., Cockcroft, J.R., Wilkinson, I.B. J. Am. Coll. Cardiol. (2003) [Pubmed]
  32. The potential contribution of endothelin-1 to neurovascular abnormalities in streptozotocin-diabetic rats. Cameron, N.E., Dines, K.C., Cotter, M.A. Diabetologia (1994) [Pubmed]
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