Showing results 61 to 80 of 215
 Comparaison de l’effet de deux coumarines sur l’inhibition de l’invasion cellulaire in vitro et in vivo; ; et al Poster (2001, January 26) Detailed reference viewed: 1 (0 ULg) Novel inhibitors of the sodium-calcium exchanger: benzene ring analogues of N-guanidino substituted amiloride derivatives; ; et al in European Journal of Medicinal Chemistry (2001), 36 Detailed reference viewed: 8 (2 ULg)Evaluation of classical NSAIDs and COX-2 selective inhibitors on purified ovine enzymes and human whole blood; ; et al in Prostaglandins, Leukotrienes, and Essential Fatty Acids (2001), 64 Detailed reference viewed: 8 (0 ULg)Pharmacology of the Thromboxane Receptor Antagonist and Thromboxane Synthase Inhibitor Bm-531; ; et al in Cardiovascular Drug Reviews (2001), 19(2, Summer), 87-96 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 ... [more ▼] 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. [less ▲] Detailed reference viewed: 10 (0 ULg)Inhibition of cellular invasion by 3-chlorophenyl 6-(acetoxymethyl)-2-oxo-2H-1-benzopyran-3-carboxylate; ; et al Poster (2000, September) Detailed reference viewed: 1 (0 ULg)Oxobenzopyran derivatives as thrombin inhibitors; ; et al Poster (2000, September) Detailed reference viewed: 1 (0 ULg)Specific inhibitors of human leukocyte elastase; ; et al Poster (2000, August) Detailed reference viewed: 3 (0 ULg)Activity and inhibition mechanism of coumarin-based derivatives as protease inhibitor; ; et al Poster (2000, June) Detailed reference viewed: 3 (0 ULg)Evaluation de la selectivité COX-1/COX-2 de drogues à visée anti-inflammatoire sur sang humain; ; et al Poster (2000, May) Detailed reference viewed: 3 (0 ULg)Conception, synthèse et évaluation pharmacologique de l’analogue pyridinique du nimésulide en tant qu’inhibiteur des cyclooxygénases; ; et al Poster (2000, May) Detailed reference viewed: 1 (0 ULg)Le 6-(acetoxymethyl)-2-oxo-2H-1-benzopyrane-3-carboxylate de 3-chlorophényle agissant en tant qu’inhibiteur potentiel de l’invasion tumorale; ; et al Poster (2000, May) Detailed reference viewed: 10 (0 ULg)Pharmacological evaluation of original sulfonylureas as thromboxane A2 antagonists; ; et al Poster (2000, March 04) Evaluation of classical NSAIDs in a model of human whole blood assay; ; et al Poster (2000, March 04) Detailed reference viewed: 1 (0 ULg)Les esters de l’acide 6-(acétoxyméthyl)-2-oxo-2H-1-benzopyrane-3-carboxylique en tant qu’agents antiinvasifs potentiels dans le traitement du cancer; ; et al Conference (2000, January 28) Detailed reference viewed: 2 (0 ULg)Les esters de l’acide 6-(acétoxyméthyl)-2-oxo-2H-1-benzopyrane-3-carboxylique en tant qu’agents antiinvasifs potentiels dans le traitement du cancer; ; et al Poster (2000, January 28) Detailed reference viewed: 3 (0 ULg)Profile of nimesulide and nimesulide-L-lysine-β-cyclodextrin on chondrocyte metabolism; ; et al in Fundamental & Clinical Pharmacology (2000), 14 Detailed reference viewed: 4 (0 ULg)Comparison of the effects of nimesulide and nimesulide-L-lysine on PGE2 production by COX-1 and COX-2 and on chondrocyte metabolism in vitro; ; et al in Pharmacy and Pharmacology Communications (2000), 6 Detailed reference viewed: 2 (2 ULg)Inhibition of cellular invasion by 3-chlorophenyl 6-(acetoxymethyl)-2-oxo-2H-1-benzopyran-3-carboxylate; ; et al in Pflügers Archiv : European Journal of Physiology (2000), 439 Detailed reference viewed: 3 (3 ULg)Evaluation of classical NSAIDs on COX-1 and COX-2 purified enzymes and prognosis of their effects on physiological responses; ; et al in Fundamental & Clinical Pharmacology (2000), 14 Detailed reference viewed: 2 (0 ULg)Characterization of antiplatelet activity of ticlopidine and acetylsalicylic acid by PFA-100; ; et al in Fundamental & Clinical Pharmacology (2000), 14 Detailed reference viewed: 11 (0 ULg) |
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