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Chemical Compound Review

SQ-28053     (Z)-7-[(1R,4S,5S,6R)-5-[(2...

Synonyms: SQ-29548, SQ29548, SQ 28053, SQ 29548, [3H]SQ-28053, ...
 
 
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Disease relevance of SQ 28053

  • TxB2 and 6-keto-PGF1 alpha, measured in blood samples obtained from the coronary artery distal to the thrombus, were significantly increased at reperfusion and at reocclusion in control animals and in dogs receiving SQ 29548 [1].
  • Infusion of papaverine to maintain stable pulmonary artery (PA) pressures, incubation of G-6-PD-inhibited platelets with acetylsalicylate, or infusion of a thromboxane-prostaglandin endoperoxide receptor site antagonist, SQ 29548, into the lung perfusate prevented augmentation of lung edema and the PA pressor response by G-6-PD-inhibited platelets [2].
  • The recovery of force generation of IMA, but not RA, upon reoxygenation after 30 min of hypoxia was significantly reduced in the initial phase of reoxygenation by indomethacin and SQ-29548 and by endothelin receptor blocker BQ-123 [cyclo(l-Leu-d-Trp-d-Asp-l-Pro-d-Val)] [3].
  • GBS-induced pulmonary hypertension could be reversed by SQ 29548; SRI 63072 did not affect PPA when administered to pigs with GBS-induced elevation in PPA [4].
  • The response was receptor specific since arrhythmias were absent after pretreatment with a specific TxA(2) receptor antagonist (SQ-29548) and did not occur in response to another prostaglandin, PGF(2alpha) [5].
 

High impact information on SQ 28053

 

Chemical compound and disease context of SQ 28053

 

Biological context of SQ 28053

 

Anatomical context of SQ 28053

 

Associations of SQ 28053 with other chemical compounds

  • Indomethacin and SQ 29548 had identical actions, preventing the decrease of GFR and antinatriuresis evoked by hyperchloremia, e.g., sodium excretion rate in the SQ 29548 and indomethacin groups increased to 7.2 +/- 1.3 and 7.1 +/- 1.2 microEq/min, respectively, compared with 2.6 +/- 0.7 microEq/min in the control group [23].
  • In contrast to control tissue, indomethacin (10 microm), the COX-2 inhibitor NS 398 (10 microm), the TXA2/PGH2 receptor antagonist SQ 29548 (1 microm) and the TXA2 synthase inhibitor furegrelate (1 microm) reduced 5-HT contraction of LPS-treated arteries from hour one [24].
  • Both TXA2 synthase inhibitor furegrelate (Fureg) and TXA2 receptor antagonist SQ-29548 (SQ) substantially blocked enhanced increase of PP in the LPS group (4.9 +/- 0.4 vs. 3.6 +/- 0.5 vs. 2.6 +/- 0.6 mmHg for LPS alone, LPS + Fureg, and LPS + SQ, respectively; P < 0.05) while having no significant effect on controls [25].
  • Dazoxiben (a pure TX synthase inhibitor) and SQ 29548 (a pure TXA2 receptor antagonist) did not affect cyclic AMP levels in AA-treated platelets.(ABSTRACT TRUNCATED AT 250 WORDS)[26]
  • We found that the IL-1-induced increase in contraction in response to ANG II was completely inhibited by 10(-5) M of the cyclooxygenase inhibitor indomethacin and also by 10(-5) M of the prostaglandin H2/thromboxane A2-receptor antagonist SQ-29548 [27].
 

Gene context of SQ 28053

 

Analytical, diagnostic and therapeutic context of SQ 28053

  • The effects of a thromboxane A2 (TxA2)-endoperoxide receptor antagonist, SQ 29548, on jejunal blood flow, oxygen uptake, and capillary filtration coefficient (Kfc) were determined in anesthetized dogs under resting conditions and during the presence of predigested food in the jejunal lumen in three series of experiments [33].
  • The stable TX mimetic U-46619 caused a dose-dependent increase in perfusion pressure that was inhibited by the TX receptor antagonist SQ 29548 [34].
  • In series 1, 2.0 micrograms intra-arterial administration of SQ 29548 was found to abolish completely the vasoconstrictor action of graded doses (0.05-2.0 micrograms) of intra-arterial injection of a TxA2-endoperoxide analogue, U44069 [33].

References

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  2. Human platelets modulate edema formation in isolated rabbit lungs. Heffner, J.E., Cook, J.A., Halushka, P.V. J. Clin. Invest. (1989) [Pubmed]
  3. Role of prostaglandins in mediating differences in human internal mammary and radial artery relaxation elicited by hypoxia. Gupte, S.A., Zias, E.A., Sarabu, M.R., Wolin, M.S. J. Pharmacol. Exp. Ther. (2004) [Pubmed]
  4. Roles of platelet-activating factor and thromboxane in group B Streptococcus-induced pulmonary hypertension in piglets. Pinheiro, J.M., Pitt, B.R., Gillis, C.N. Pediatr. Res. (1989) [Pubmed]
  5. Thromboxane A2-induced arrhythmias in the anesthetized rabbit. Wacker, M.J., Best, S.R., Kosloski, L.M., Stachura, C.J., Smoot, R.L., Porter, C.B., Orr, J.A. Am. J. Physiol. Heart Circ. Physiol. (2006) [Pubmed]
  6. Increased thromboxane mediates the adverse renal effects of interleukin-2 in rats. Rubinger, D., Cohen, E., Haviv, Y., Bernheim, J., Shiloni, E., Popovtzer, M.M. J. Am. Soc. Nephrol. (1994) [Pubmed]
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  8. COX-2 up-regulation and vascular smooth muscle contractile hyperreactivity in spontaneous diabetic db/db mice. Guo, Z., Su, W., Allen, S., Pang, H., Daugherty, A., Smart, E., Gong, M.C. Cardiovasc. Res. (2005) [Pubmed]
  9. H2O2 increases production of constrictor prostaglandins in smooth muscle leading to enhanced arteriolar tone in Type 2 diabetic mice. Erdei, N., Bagi, Z., Edes, I., Kaley, G., Koller, A. Am. J. Physiol. Heart Circ. Physiol. (2007) [Pubmed]
  10. Chronic hyperglycemia impairs functional vasodilation via increasing thromboxane-receptor-mediated vasoconstriction. Xiang, L., Naik, J.S., Abram, S.R., Hester, R.L. Am. J. Physiol. Heart Circ. Physiol. (2007) [Pubmed]
  11. Altered arachidonic acid metabolism impairs functional vasodilation in metabolic syndrome. Xiang, L., Naik, J.S., Hodnett, B.L., Hester, R.L. Am. J. Physiol. Regul. Integr. Comp. Physiol. (2006) [Pubmed]
  12. The role of the central thromboxane A2 in cardiovascular effects of a phospholipase A2 activator melittin administrated intracerebroventricularly in normotensive conscious rats. Yalcin, M., Ak, F., Erturk, M. Neuropeptides (2006) [Pubmed]
  13. Effects of TRA-418, a novel TP-receptor antagonist, and IP-receptor agonist, on human platelet activation and aggregation. Miyamoto, M., Yamada, N., Ikezawa, S., Ohno, M., Otake, A., Umemura, K., Matsushita, T. Br. J. Pharmacol. (2003) [Pubmed]
  14. Thromboxane A2 agonist modulation of excitatory synaptic transmission in the rat hippocampal slice. Hsu, K.S., Kan, W.M. Br. J. Pharmacol. (1996) [Pubmed]
  15. Protein kinase C-zeta modulates thromboxane A(2)-mediated apoptosis in adult ventricular myocytes via Akt. Shizukuda, Y., Buttrick, P.M. Am. J. Physiol. Heart Circ. Physiol. (2002) [Pubmed]
  16. Thromboxane A2-mimetics are potent microvascular permeability factors in the conjunctiva. Woodward, D.F., Nieves, A.L., Williams, L.S. J. Pharmacol. Exp. Ther. (1990) [Pubmed]
  17. Cyclooxygenase inhibition prevents PMA-induced increases in lung vascular permeability. Zanaboni, P.B., Bradley, J.D., Baudendistel, L.J., Webster, R.O., Dahms, T.E. J. Appl. Physiol. (1990) [Pubmed]
  18. The bovine thromboxane A2 receptor: molecular cloning, expression, and functional characterization. Muck, S., Weber, A.A., Meyer-Kirchrath, J., Schrör, K. Naunyn Schmiedebergs Arch. Pharmacol. (1998) [Pubmed]
  19. Protective actions of a thromboxane receptor antagonist, SQ 29548 on the ischemic myocardium: morphologic and hemodynamic effects. Singh, J., Seth, S.D., Manchanda, S.C., Seth, S. Prostaglandins Leukot. Essent. Fatty Acids (1997) [Pubmed]
  20. Time-dependent hyperreactivity to phenylephrine in aorta from untreated diabetic rats: role of prostanoids and calcium mobilization. Xavier, F.E., Davel, A.P., Rossoni, L.V., Vassallo, D.V. Vascul. Pharmacol. (2003) [Pubmed]
  21. Stimulation of rat mesangial cell thromboxane A2 receptors inhibits particulate but not soluble guanylyl cyclase. Paul, R.V., Saxenhofer, H., Wackym, P.S., Halushka, P.V. Am. J. Physiol. (1996) [Pubmed]
  22. Role of superoxide anion and endothelium in vasoconstrictor action of prostaglandin endoperoxide. Tesfamariam, B., Cohen, R.A. Am. J. Physiol. (1992) [Pubmed]
  23. Analysis of eicosanoid mediation of the renal functional effects of hyperchloremia. Askari, B., Bell-Quilley, C.P., Fulton, D., Quilley, J., McGiff, J.C. J. Pharmacol. Exp. Ther. (1997) [Pubmed]
  24. Mechanisms involved in the early increase of serotonin contraction evoked by endotoxin in rat middle cerebral arteries. Hernanz, R., Alonso, M.J., Briones, A.M., Vila, E., Simonsen, U., Salaices, M. Br. J. Pharmacol. (2003) [Pubmed]
  25. Thromboxane A2 from Kupffer cells contributes to the hyperresponsiveness of hepatic portal circulation to endothelin-1 in endotoxemic rats. Xu, H., Korneszczuk, K., Karaa, A., Lin, T., Clemens, M.G., Zhang, J.X. Am. J. Physiol. Gastrointest. Liver Physiol. (2005) [Pubmed]
  26. Pharmacological characterization of cinnamophilin, a novel dual inhibitor of thromboxane synthase and thromboxane A2 receptor. Yu, S.M., Wu, T.S., Teng, C.M. Br. J. Pharmacol. (1994) [Pubmed]
  27. Effects of tumor necrosis factor and interleukin-1 on the constriction induced by angiotensin II in rat aorta. Vicaut, E., Rasetti, C., Baudry, N. J. Appl. Physiol. (1996) [Pubmed]
  28. Modulation of noradrenaline-induced vasoconstriction in isolated perfused mesenteric arterial beds from obese Zucker rats in the presence and absence of insulin. He, Y., MacLeod, K.M. Can. J. Physiol. Pharmacol. (2002) [Pubmed]
  29. Different effects of endothelin-3 on the Ca2+ discharge induced by agonists and Ca(2+)-ATPase inhibitors in human platelets. Astarie-Dequeker, C., Korichneva, I., Devynck, M.A. Br. J. Pharmacol. (1995) [Pubmed]
  30. Lipid peroxidation increases arterial cyclooxygenase activity during pregnancy. Davidge, S.T., Hubel, C.A., McLaughlin, M.K. Am. J. Obstet. Gynecol. (1994) [Pubmed]
  31. Mast cell degranulation alters lymphatic contractile activity through action of histamine. Plaku, K.J., von der Weid, P.Y. Microcirculation (New York, N.Y. : 1994) (2006) [Pubmed]
  32. Angiotensin II constriction of rat vasa recta is partially thromboxane dependent. Silldorff, E.P., Hilbun, L.R., Pallone, T.L. Hypertension (2002) [Pubmed]
  33. Thromboxane plays a role in postprandial jejunal oxygen uptake and capillary exchange. Alemayehu, A., Chou, C.C. Am. J. Physiol. (1990) [Pubmed]
  34. Evidence for functional thromboxane A2-prostaglandin H2 receptors in human placenta. Hedberg, A., Mento, P.F., Liu, E.C., Hollander, A.M., Wilkes, B.M. Am. J. Physiol. (1989) [Pubmed]
 
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