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Chemical Compound Review

DALTROBAN     2-[4-[2-[(4-chlorophenyl) sulfonylamino]eth...

Synonyms: Daltrobanum, CHEMBL71685, SureCN309160, D7441_SIGMA, SKF-96148, ...
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Disease relevance of DALTROBAN


High impact information on DALTROBAN


Chemical compound and disease context of DALTROBAN


Biological context of DALTROBAN

  • The extent of thromboxane antagonism achieved with SQ 30,741 (50 and 500 micrograms/kg/min) and BM 13,505 (50 micrograms/kg/min) was determined from parallel shifts in dose-dependent U-46,619-induced vasoconstriction in vivo (approximately 200- and 1300-fold, respectively, for SQ 30,741 and 200-fold for BM 13,505) [2].
  • BM-13505 significantly (p less than 0.001) reduced the area of ischemic tissue as a percent of total left ventricular mass and total area at risk, without altering basic hemodynamics (i.e., arterial blood pressure, heart rate, or their product) and thereby not influencing myocardial oxygen demand [4].
  • The rank orders of potency of these antagonists, which correlated well between human (h) and canine (c) preparations were [IC50]: SQ 29,548 [28 nM (h) and 92 nM (c)] greater than AH 23,848 [0.5 microM (h) and 0.6 microM (c)] congruent to BM 13.505 [0.4 microM (h) and 0.8 microM (c)] greater than BM 13.177 [3.9 microM (h) and 4.4 microM (c)] [12].
  • SAO shock rats treated with BM-13505 (1 mg/kg) maintained post-reperfusion mean arterial blood pressure (MABP) at significantly higher values compared to those receiving only the vehicle (0.9% NaCl) [13].
  • Thus, the beneficial effects of BM-13505 in hemorrhagic shock are likely due to both its prevention of thromboxane-induced vasoconstriction and its ability to attenuate thromboxane-induced platelet aggregation [14].

Anatomical context of DALTROBAN


Associations of DALTROBAN with other chemical compounds


Gene context of DALTROBAN

  • Pretreatment of the animals with BM-13505 (1 mg/kg), a thromboxane A2 (TxA2) receptor antagonist, prolonged the duration of the hypotensive response to ET-1 (1.0 nmol/kg) but had no effect on the pressor response [23].
  • We compared the abilities of four TXA2/PGH2 receptor antagonists, AH 23,848, SQ 29,548, BM 13.177 and BM 13.505, to inhibit aggregation of human and canine platelet rich plasma (PRP) induced by the stable cyclic endoperoxide analog, U46619, alone (human) or in combination with epinephrine (dog) [12].
  • Treatment with BM-13505 attenuated the plasma activity of the lysosomal protease cathepsin D (p less than 0.05 from vehicle) and the plasma accumulation of free amino-nitrogen compounds (p less than 0.01 from vehicle) [13].

Analytical, diagnostic and therapeutic context of DALTROBAN

  • BM-13505 or its vehicle (i.e., Na2CO3) was administered intravenously 30 minutes before reperfusion at a rate of 1 mg/kg followed by 1 mg/kg/hr [4].


  1. Lack of involvement of thromboxane A2 in postischemic recovery of stunned canine myocardium. Farber, N.E., Pieper, G.M., Gross, G.J. Circulation (1988) [Pubmed]
  2. Effect of thromboxane receptor antagonists on venous thrombosis in rats. Schumacher, W.A., Heran, C.L. J. Pharmacol. Exp. Ther. (1989) [Pubmed]
  3. Severe VA/Q mismatch in perfused lungs evoked by sequential challenge with endotoxin and E. coli hemolysin. Walmrath, D., Pilch, J., Scharmann, M., Grimminger, F., Seeger, W. J. Appl. Physiol. (1994) [Pubmed]
  4. Protective effect of the specific thromboxane receptor antagonist, BM-13505, in reperfusion injury following acute myocardial ischemia in cats. Bhat, A.M., Sacks, H., Osborne, J.A., Lefer, A.M. Am. Heart J. (1989) [Pubmed]
  5. Influence of SK&F 96148 on thromboxane-mediated responses in the airways of the cat. Dyson, M.C., Kadowitz, P.J. Eur. J. Pharmacol. (1991) [Pubmed]
  6. Thromboxane synthase inhibition enhances action of converting enzyme inhibitors. Levens, N.R., Ksander, G.M., Zimmerman, M.B., Mullane, K.M. Hypertension (1989) [Pubmed]
  7. Difference of (Ca2+)i movements in platelets stimulated by thrombin and TRAP: the involvement of alpha(IIb)beta3-mediated TXA2 synthesis. Aoki, T., Tomiyama, Y., Honda, S., Senzaki, K., Tanaka, A., Okubo, M., Takahashi, F., Takasugi, H., Seki, J. Thromb. Haemost. (1998) [Pubmed]
  8. Prostaglandin E2 inhibits noradrenaline release and purinergic pressor responses to renal nerve stimulation at 1 Hz in isolated kidneys of young spontaneously hypertensive rats. Rump, L.C., Wilde, K., Schollmeyer, P. J. Hypertens. (1990) [Pubmed]
  9. Intrinsic activity of the non-prostanoid thromboxane A2 receptor antagonist, daltroban (BM 13,505), in human platelets in vitro and in the rat vasculature in vivo. Bertolino, F., Valentin, J.P., Maffre, M., Grelac, F., Bessac, A.M., Maclouf, J., Delhon, A., Lévy-Toledano, S., Patoiseau, J.F., Colpaert, F.C. Br. J. Pharmacol. (1995) [Pubmed]
  10. Identification of a single (FP) receptor associated with prostanoid-induced Ca2+ signals in Swiss 3T3 cells. Woodward, D.F., Lawrence, R.A. Biochem. Pharmacol. (1994) [Pubmed]
  11. Staphylococcal alpha-toxin induced ventilation-perfusion mismatch in isolated blood-free perfused rabbit lungs. Walmrath, D., Scharmann, M., König, R., Pilch, J., Grimminger, F., Seeger, W. J. Appl. Physiol. (1993) [Pubmed]
  12. Antagonism of U46619-induced aggregation of human and canine platelets by four TXA2 receptor antagonists. Bush, L.R., Smith, S.G. Thromb. Res. (1986) [Pubmed]
  13. Protective effects of thromboxane receptor blockade in splanchnic artery occlusion shock. Aoki, N., Lefer, A.M. Methods and findings in experimental and clinical pharmacology. (1988) [Pubmed]
  14. Beneficial actions of thromboxane receptor antagonism in hemorrhagic shock. Bitterman, H., Yanagisawa, A., Lefer, A.M. Circ. Shock (1986) [Pubmed]
  15. Interspecies differences in thromboxane receptors: studies with thromboxane receptor antagonists in rat and guinea pig smooth muscles. Ogletree, M.L., Allen, G.T. J. Pharmacol. Exp. Ther. (1992) [Pubmed]
  16. BM 13.505, a selective thromboxane receptor antagonist, reduces myocardial infarct size following coronary artery reperfusion. Smith, E.F., Earl, C.Q., Egan, J.W. Prostaglandins Leukot. Essent. Fatty Acids (1989) [Pubmed]
  17. The strong contractile effect of the thromboxane receptor agonist U-46619 in isolated human pulmonary arteries and its competitive antagonism by BM-13.505. Sjöberg, T., Steen, S. Acta Physiol. Scand. (1989) [Pubmed]
  18. Reduction of myocardial damage and polymorphonuclear leukocyte accumulation following coronary artery occlusion and reperfusion by the thromboxane receptor antagonist BM 13.505. Smith, E.F., Griswold, D.E., Egan, J.W., Hillegass, L.M., DiMartino, M.J. J. Cardiovasc. Pharmacol. (1989) [Pubmed]
  19. Induction of cyclic flow reduction in the coronary, carotid, and femoral arteries of conscious, chronically instrumented dogs. A model for investigating the role of platelets in severely constricted arteries. Al-Wathiqui, M.H., Hartman, J.C., Brooks, H.L., Warltier, D.C. Journal of pharmacological methods. (1988) [Pubmed]
  20. Constriction of cat coronary arteries by synthetic thromboxane A2 and its antagonism. Smith, J.B., Yanagisawa, A., Zipkin, R., Lefer, A.M. Prostaglandins (1987) [Pubmed]
  21. Endothelium dependence of prostanoid-induced relaxation in human hand veins. Arner, M., Uski, T., Högestätt, E.D. Acta Physiol. Scand. (1994) [Pubmed]
  22. Cardioprotective actions of thromboxane receptor antagonism in ischemic atherosclerotic rabbits. Osborne, J.A., Lefer, A.M. Am. J. Physiol. (1988) [Pubmed]
  23. Endothelin-1 enhances vascular permeability in conscious rats: role of thromboxane A2. Sirois, M.G., Filep, J.G., Rousseau, A., Fournier, A., Plante, G.E., Sirois, P. Eur. J. Pharmacol. (1992) [Pubmed]
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