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Pharmacology of the thromboxane receptor antagonist and thromboxane synthase inhibitor BM-531 Dogne JM; Rolin S; de Leval X; Benoit P; Neven P; Delarge J; Kolh P; Damas J; David JL; Masereel BCardiovasc Drug Rev 2001[Sum]; 19 (2): 87-96BM-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.|Animals[MESH]|Blood Platelets/drug effects/metabolism[MESH]|Diuresis/drug effects[MESH]|Enzyme Inhibitors/metabolism/*pharmacology[MESH]|Gastric Fundus/drug effects/physiology[MESH]|Humans[MESH]|Muscle Contraction/drug effects/physiology[MESH]|Muscle, Smooth/drug effects/physiology[MESH]|Platelet Aggregation Inhibitors/metabolism/*pharmacology[MESH]|Radioligand Assay[MESH]|Receptors, Thromboxane/*antagonists & inhibitors/metabolism[MESH]|Sulfonamides/pharmacology[MESH]|Sulfonylurea Compounds/metabolism/*pharmacology[MESH]|Thromboxane A2/biosynthesis/*metabolism[MESH]|Thromboxane-A Synthase/*antagonists & inhibitors[MESH]|Torsemide[MESH] |
