Reference : Pharmacology of the Thromboxane Receptor Antagonist and Thromboxane Synthase Inhibitor B...
Scientific journals : Article
Human health sciences : Cardiovascular & respiratory systems
http://hdl.handle.net/2268/15690
Pharmacology of the Thromboxane Receptor Antagonist and Thromboxane Synthase Inhibitor Bm-531
English
Dogné, J. M. [ > > ]
Rolin, S. [> > > >]
de Leval, X. [ > > ]
Benoit, P. [> > > >]
Neven, P. [> > > >]
Delarge, J. [> > > >]
Kolh, Philippe mailto [Université de Liège - ULg > Département des Sciences biomédicales et précliniques > Service de Biochimie et de Physiologie générales, humaines, normales et pathologiques > >]
Damas, Jacques mailto [Université de Liège - ULg > Département des sciences biomédicales et précliniques > Département des sciences biomédicales et précliniques >]
David, Jean-Louis [Université de Liège - ULg > Services généraux (Faculté de médecine) > Relations académiques et scientifiques (Médecine) >]
Masereel, B. [> > > >]
2001
Cardiovascular Drug Reviews
19
2, Summer
87-96
Yes (verified by ORBi)
International
0897-5957
[en] BM-531 (N-tert-butyl-N'-[(2-cyclohexylamino-5-nitrobenzene)sulfonyl]urea), a torasemide derivative, is a novel noncarboxylic thromboxane receptor antagonist and thromboxane synthase inhibitor. Indeed, its affinity for human washed platelet TXA2 receptors labeled with [3H]SQ-29548 (IC50 = 0.0078 microM) is higher than sulotroban (IC50 = 0.93 microM) and SQ-29548 (IC50 = 0.021 microM). Moreover, BM-531 is characterized by a potent antiaggregatory property. Indeed, on one hand, in human citrated platelet-rich plasma BM-531 prevents platelet aggregation induced by arachidonic acid (600 microM) (ED100 = 0.125 microM), U-46619, a stable TXA2 agonist (1 microM) (ED50 = 0.482 microM) or collagen (1 microgram/mL) (percentage of inhibition: 42.9% at 10 microM) and inhibits the second wave of ADP (2 microM)-induced aggregation. On the other hand, when BM-531 is incubated in whole blood from healthy donors, the closure time measured by the recently developed platelet function analyser (PFA-100) is significantly prolonged. In addition, at the concentrations of 10 and 1 microM, BM-531 totally prevents the production of TXB2 by human platelets activated by arachidonic acid. Finally, at 10 microM, BM-531 significantly prevents rat fundus contractions induced by U-46619 but not by prostacyclin. These results suggest that BM-531, which is devoid of the diuretic property of torasemide, can be regarded as a promising antiplatelet agent.
http://hdl.handle.net/2268/15690

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