Pharmacological profile and therapeutic potential of BM-573, a combined thromboxane receptor antagonist and synthase inhibitor

Cardiovascular Drug Reviews

Volumn 23, Issue 1, 2005, Pages 1-14

  Ghuysen, Alexandre ^a,c   Dogné, Jean Michel ^a   Chiap, Patrice ^a   Rolin, Stéphanie ^b   Masereel, Bernard ^b   Lambermont, Bernard ^a   Kolh, Philippe ^a   Tchana Sato, Vincent ^a   Hanson, Julien ^a   D'Orio, Vincent ^a  

^a UNIVERSITY OF LIÈGE   (Belgium)

^b UNIVERSITY OF NAMUR   (Belgium)

^c UNIVERSITY OF LIÈGE   (Belgium)

Author keywords

Antiplatelet agents; BM 573; Thromboxane antagonists; Thromboxane synthase inhibitors

Indexed keywords

15 HYDROXY 11ALPHA,9ALPHA EPOXYMETHANOPROSTA 5,13 DIENOIC ACID; 7 [3 [(4 PHENYLSEMICARBAZIDO)METHYL] 7 OXABICYCLO[2.2.1]HEPT 2 YL] 5 HEPTENOIC ACID; ACETYLSALICYLIC ACID; ANTITHROMBOCYTIC AGENT; ARACHIDONIC ACID; BM 573; FERRIC CHLORIDE; FUREGRELATE; GLIBENCLAMIDE; GLUCOSE; N TERT BUTYL N' [2 (4' METHYLPHENYLAMINO) 5 NITROBENZENESULFONYL]UREA; PROSTACYCLIN; PROSTAGLANDIN; SERATRODAST; SULFONYLUREA DERIVATIVE; SULOTROBAN; THROMBOXANE A2 RECEPTOR BLOCKING AGENT; THROMBOXANE B2; THROMBOXANE SYNTHASE INHIBITOR; TICLOPIDINE; TORASEMIDE; TORASEMIDE DERIVATIVE; UNCLASSIFIED DRUG;

ABDOMINAL AORTA; AORTA OCCLUSION; BLEEDING TIME; CONCENTRATION RESPONSE; CORONARY ARTERY THROMBOSIS; DEVICE; DISEASE MODEL; DOG; DRUG EFFECT; DRUG STRUCTURE; GLUCOSE BLOOD LEVEL; GUINEA PIG; HEART INFARCTION; HUMAN; LUNG EMBOLISM; MUSCLE CONTRACTION; NONHUMAN; PRIORITY JOURNAL; PULMONARY HYPERTENSION; RAT; RECEPTOR AFFINITY; REVIEW; SEPTIC SHOCK; STRUCTURE ANALYSIS; SWINE; THROMBOCYTE ACTIVATION; THROMBOCYTE AGGREGATION INHIBITION; THROMBOCYTE FUNCTION; THROMBUS; TRACHEA MUSCLE;

EID: 20244367317     PISSN: 08975957     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.1527-3466.2005.tb00153.x     Document Type: Review

References (51)

1. 2. Nature 1985;315:511-513.
2. Brezinski ME, Yanagisawa A, Lefer AM. Cardioprotective actions of specific thromboxane receptor antagonist in acute myocardial ischemia. J Cardiovasc Pharmacol 1987;9:65-71.
3. 2 receptor in dog coronary artery in vitro. Br J Pharmacol 1990;100:375-378.
4. 2 on some isolated smooth muscle preparations. Br J Pharmacol 1981;73:773-778.
5. Collins BJ, Blum MG, Parker RE, et al. Thromboxane mediates pulmonary hypertension and lung inflammation during hyperacute lung rejection. J Appl Physiol 2001;90:2257-2268.
6. D'Orio V, Lambermont B, Detry O, et al. Pulmonary impedance and right ventricular-vascular coupling in endotoxin shock. Cardiovasc Res 1998;38:375-382.
7. 2/prostaglandin endoperoxide receptor blockade combined in one molecule. II. Pharmacological effects in vivo and ex vivo. Thromb Haemost 1989;61:43-49.
8. Dogne JM, de Leval, X, Kolh P, et al. Pharmacological evaluation of the novel thromboxane modulator BM-567 (I/II). Effects of BM-567 on platelet function. Prostaglandins Leukot Essent Fatty Acids 2003;68: 49-54.
9. 2 receptor antagonist (BM-531) derived from torasemide on platelet function. Prostaglandins Leukot Essent Fatty Acids 2000;62:311-317.
10. 2 receptor antagonist and thromboxane synthase inhibitor in a rat model of arterial thrombosis and its effects on bleeding time. J Pharmacol Exp Ther 2004;309:498-505.
11. 2 receptor antagonist and thromboxane synthase inhibitor. J Pharm Pharmacol 2001; 53:669-680.
12. Eikelboom JW, Hirsh J, Weitz JI, Johnston M, Yi Q, Yusuf S. Aspirin-resistant thromboxane biosynthesis and the risk of myocardial infarction, stroke, or cardiovascular death in patients at high risk for cardiovascular events. Circulation 2002;105:1650-1655.
13. 2. Science 1976;193:1135-1137.
14. Fiddler GI, Lumley P. Preliminary clinical studies with thromboxane synthase inhibitors and thromboxane receptor blockers. A review. Circulation 1990;81:169-178.
15. Fishbein MC, Meerbaum S, Rit J, et al. Early phase acute myocardial infarct size quantification: Validation of the triphenyl tetrazolium chloride tissue enzyme staining technique. Am Heart J 1981;101:593-600.
16. Fitzgerald DJ, Roy L, Catella F, Fitzgerald GA. Platelet activation in unstable coronary disease. N Engl J Med 1986;315:983-989.
17. Ghuysen A, Lambermont B, Dogné JM, et al. Effect of BM-573 [N-terbutyl-N′-[2-(4′-methylphenyl-amino)-5-nitro-benzenesulfonyl] urea], a dual thromboxane synthase inhibitor and thromboxane receptor antagonist, in a porcine model of acute pulmonary embolism. J Pharmacol Exp Ther 2004;310:964-972.
18. 2: Biosynthesis and effects on platelets. Adv Prostaglandin Thromboxane Leukot Res 1982;10:15-58.
19. Hamberg M, Svensson J, Samuelsson B. Thromboxanes: A new group of biologically active compounds derived from prostaglandin endoperoxides. Proc Natl Acad Sci USA 1975;72:2994-2998.
20. Hamberg M, Svensson J, Wakabayashi T, Samuelsson B. Isolation and structure of two prostaglandin endoperoxides that cause platelet aggregation. Proc Natl Acad Sci USA 1974;71:345-349.
21. Hamm CW, Lorenz RL, Bleifeld W, Kupper W, Wober W, Weber PC. Biochemical evidence of platelet activation in patients with persistent unstable angina. J Am Coll Cardiol 1987;10:998-1006.
22. 2 per PG-END receptor antagonist. Blood Coagul Fibrinolysis 1991;2:617-621.
23. Hirsh PD, Firth BG, Campbell WB, Dehmer GJ, Willerson JT, Hillis LD. Effects of provocation on transcardiac thromboxane in patients with coronary artery disease. Am J Cardiol 1983;51:727-733.
24. Hirsh PD, Hillis LD, Campbell WB, Firth BG, Willerson JT. Release of prostaglandins and thromboxane into the coronary circulation in patients with ischemic heart disease. N Engl J Med 1981;304:685-691.
25. Hock CE, Brezinski ME, Lefer AM. Anti-ischemic actions of a new thromboxane receptor antagonist, SQ-29,548, in acute myocardial ischemia. Eur J Pharmacol 1986;122:213-219.
26. 2 receptor antagonist, on airway inflammation in subjects with asthma. J Allergy Clin Immunol 1999;103:1054-1061.
27. Imamoto T, Terashita Z, Tanabe M, Nishikawa K, Hirata M. Protective effect of a novel thromboxane synthetase inhibitor, CV-4151, on myocardial damage due to coronary occlusion and reperfusion in the hearts of anesthetized dogs. J Cardiovasc Pharmacol 1986;8:832-839.
28. Kundu SK, Heilmann EJ, Sio R, Garcia C, Davidson RM, Ostgaard RA. Description of an in vitro platelet function analyzer - PFA-100. Semin Thromb Hemost 1995;21(Suppl 2):106-112.
29. 2 inhibitor, on pulmonary hemodynamics in endotoxic shock. Arch Physiol Biochem 2003;111:224-231.
30. Lambermont B, Ghuysen A, Kolh P, et al. Effects of endotoxic shock on right ventricular systolic function and mechanical efficiency. Cardiovasc Res 2003;59:412-418.
31. 2 inhibitor. Arch Physiol Biochem 2003;111:217-223.
32. 2 inhibitor on right ventricular-arterial coupling in endotoxic shock. Shock 2004;21:45-51.
33. + channels and inhibiting insulin release. Diabetologia 2000;43:723-732.
34. Ma H, Hara A, Xiao CY, et al. Increased bleeding tendency and decreased susceptibility to thromboembolism in mice lacking the prostaglandin E receptor subtype EP(3). Circulation 2001;104:1176-1180.
35. 2 receptor antagonism in man and rat by a sulphonylcyanoguanidine (BM-144) and a sulphonylurea (BM-500). J Pharm Pharmacol 1999;51:695-701.
36. Needleman P, Wyche A, Raz A. Platelet and blood vessel arachidonate metabolism and interactions. J Clin Invest 1979;63:345-349.
37. 2 biosynthesis in lung, spleen or platelets. Eur J Pharmacol 1977;44: 179-186.
38. Ogletree ML, Brigham KL. Effects of cyclooxygenase inhibitors on pulmonary vascular responses to endotoxin in unanesthetized sheep. Prostaglandins Leukot Med 1982;8:489-502.
39. Pawlowski NA, Kaplan G, Hamill AL, Cohn ZA, Scott WA. Arachidonic acid metabolism by human monocytes. Studies with platelet-depleted cultures. J Exp Med 1983;158:393-412.
40. 2 receptor antagonist and thromboxane synthase inhibitor (BM-573) on platelet function and isolated smooth muscles. Prostaglandins Leukot Essent Fatty Acids 2001;65:67-72.
41. Rolin S, Petein M, Tchana-Sato V, et al. BM-573, a dual thromboxane synthase inhibitor and thromboxane receptor antagonist, prevents pig myocardial infarction induced by coronary thrombosis. J Pharmacol Exp Ther 2003;306:59-65.
42. 2 by coronary arteries after thrombolysis. Am Heart J 1993;125:277-284.
43. Smulders YM. Pathophysiology and treatment of haemodynamic instability in acute pulmonary embolism: The pivotal role of pulmonary vasoconstriction. Cardiovasc Res 2000;48:23-33.
44. 2-induced contraction in human internal mammary artery and saphenous vein. Eur J Pharmacol 1998;341:65-71.
45. Stein PD and Henry JW. Prevalence of acute pulmonary embolism among patients in a general hospital and at autopsy. Chest 1995;108:978-981.
46. 2 in human platelets. Acta Physiol Scand 1976;98:285-294.
47. Tanaka T, Ito S, Higashino R, et al. A new thromboxane receptor antagonist, Z-335, ameliorates experimental thrombosis without prolonging the rat tail bleeding time. Thromb Res 1998;91:229-235.
48. 2 per prostaglandin endoperoxide receptor antagonist, versus aspirin as adjunct to thrombolysis in patients with acute myocardial infarction. The Ridogrel Versus Aspirin Patency Trial (RAPT). Circulation 1994;89:588-595.
49. 2-induced contraction in the isolated canine coronary artery. Prostaglandins Leukot Essent Fatty Acids 1992;45:121-124.
50. 2 synthase inhibition alone and in combination: comparison of anti-aggregatory efficacy in human platelets. Br J Pharmacol 1991;102:497-505.
51. 2 in the pathogenesis of endotoxic shock. Adv Shock Res 1981;6:83-91.