References of "De Leval, X."
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See detailNew trends in dual 5-LOX/COX inhibition
De Leval, X.; Julémont, F.; Delarge, J. et al

in Current Medicinal Chemistry (2002), 9

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See detailEvaluation of pyridinic sulfonamides related to nimesulide as COX-2 selective inhibitors
Julemont, F.; De Leval, X.; Neven, P. et al

in Fundamental & Clinical Pharmacology (2002)

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See detailN-(3-Phenoxy-4-pyridinio)methanesulfonamidate
Michaux, C.; Charlier, C.; Julémont, F. et al

in Acta Crystallographica (2002)

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See detailEffects of thromboxane A2 receptor antagonists and thromboxane synthase inhibitors on osteogenic sarcoma cell-induced platelet aggregation
De Leval, X.; Benoit, V.; Neven, P. et al

in Fundamental & Clinical Pharmacology (2002), 16

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See detailEvaluation of pyridinic sulfonamides related to nimesulide as COX-2 selective inhibitors
Julémont, F.; De Leval, X.; Neven, P. et al

in Fundamental & Clinical Pharmacology (2002)

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See detailEffects of BM-573, a dual thromboxane A2 receptor antagonist and thromboxane synthase inhibitor, on osteogenic sarcoma cell-induced platelet aggregation
De Leval, X.; David, J. L.; Neven, P. et al

Poster (2001, December)

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See detailSynthesis and pharmacological evaluation of pyridinic sulfonamides related to nimesulide
Julemont, F.; De Leval, X.; Neven, P. et al

Poster (2001, November 16)

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See detailEffects of BM-573, a dual thromboxane A(2) receptor antagonist and thromboxane synthase inhibitor, on osteogenic sarcoma cell-induced platelet aggregation
de Leval, X.; David, Jean-Louis ULg; Neven, P. et al

in Blood (2001, November 16), 98(11, Part 2), 43

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See detailEvaluation d’inhibiteurs de cyclooxygénases et d’antagonistes du TXA2 sur la migration des cellules endothéliales in vitro
Lux, C.; Delarge, J.; De Leval, X. et al

Poster (2001, June 01)

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See detailSynthèse et évaluation pharmacologique d’un méthanesulfonamide pyridinique apparenté à l’acide niflumique
Julemont, F.; De Leval, X.; Neven, P. et al

Poster (2001, June 01)

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See detailEffects of thromboxane A2 receptor antagonists and COX inhibitors on osteogenic sarcome cell-induced platelet aggregation
De Leval, X.; Delarge, J.; Neven, P. et al

Poster (2001, June 01)

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See detailSynthesis and pharmacological evaluation of pyridinic methanesulfonamides as potential COX-2 inhibitors
Julémont, F.; de Leval, X.; Neven, P. et al

Conference (2001, May 24)

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See detailSynthesis and pharmacological evaluation of pyridinic methanesulfonamides as potential COX-2 inhibitors
Julemont, F.; De Leval, X.; Neven, P. et al

Conference (2001, May)

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See detailConception, synthèse et évaluation pharmacologique d’analogues pyridiniques du Nimésulide en tant qu’inhibiteurs potentiels des cyclooxygénases
Julémont, Fabien; De Leval, X.; Neven, P. et al

Poster (2001, January 26)

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See detailEvaluation of classical NSAIDS and COX-2 selective inhibitors on purified ovine enzymes and human whole blood
De Leval, X; Dogne, JM; Delange, J et al

in Annals of the Rheumatic Diseases (2001), 60(S1), 343

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See detailEvaluation of classical NSAIDS and COX-2 selective inhibitors on purified ovine enzymes and human whole blood
de Leval, X; Dogne, JM; Delarge, J et al

in Clinical Rheumatology (2001), 20

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See detailIn vitro effects of aceclofenac and its metabolites on the production by chondrocytes of inflammatory mediators.
Henrotin, Yves ULg; de Leval, X.; Mathy, Marianne ULg et al

in Inflammation Research (2001), 50(8), 391-9

OBJECTIVES: To investigate the mechanisms of action underlying the anti-inflammatory action of aceclofenac in vivo, we studied in vitro the effect of aceclofenac and its main metabolite, 4 ... [more ▼]

OBJECTIVES: To investigate the mechanisms of action underlying the anti-inflammatory action of aceclofenac in vivo, we studied in vitro the effect of aceclofenac and its main metabolite, 4'-hydroxyaceclofenac, in comparison with diclofenac, another metabolite, on cyclooxygenases activity as well as interleukin-1beta, -6 and -8, nitric oxide, and prostaglandin E2 production by human osteoarthritic and normal articular chondrocytes. METHODS: Enzymatically isolated human chondrocytes were cultured for 72 h in the absence or presence of interleukin-1beta (IL-1beta) or lipopolysacharride (LPS) and with or without increased amounts (1 to 30 microM) of aceclofenac or metabolites. The production of different cytokines was measured by Enzyme Amplified Sensitivity Immunoassays (EASIA). Prostaglandin E2 was quantified by a specific radioimmunoassay. Nitrite and nitrate concentrations in the culture supernatants were determined by spectrophotometric method based upon the Griess reaction. Cyclooxygenase-2, inducible NO synthase and IL-1beta gene expression were quantified by reverse transcription of mRNA followed by real time and quantitative polymerase chain reaction. Finally, cyclooxygenase inhibitory potency of the drugs was also tested in both a cell-free system using purified ovine cyclooxygenase-1 and -2 (COX-1 and COX-2) and at a cellular level using human whole blood assay. RESULTS: We have demonstrated that aceclofenac, 4'-hydroxyaceclofenac and diclofenac significantly decreased interleukin-6 production at concentrations ranged among 1 to 30 microM and fully blocked prostaglandin E2 synthesis by IL-1beta- or LPS-stimulated human chondrocytes. Aceclofenac and diclofenac had no effect on interleukin-8 production while 4'-hydroxyaceclofenac slightly decreased this parameter at the highest dose (30 microM). Aceclofenac was without effect on IL-1beta- or LPS-stimulated nitric oxide production. At 30 microM, 4'-hydroxyaceclofenac inhibited both IL-1beta or LPS-stimulated nitric oxide production while diclofenac inhibited only the LPS-stimulated production. Finally, at 30 microM, the three drugs significantly decreased IL-1beta mRNA. In the whole blood test, aceclofenac and 4'-hydroxyaceclofenac weakly inhibited COX-1 with IC50 values superior to 100 microM, but decreased by 50% COX-2 activity at the concentration of 0.77 and 36 microM, respectively. Diclofenac strongly inhibited both COX-1 and COX-2 with IC50 values of 0.6 and 0.04 microM, respectively. On the other hand, aceclofenac and diclofenac weakly inhibited purified ovine cyclooxygenases with IC50 values superior to 100 microM, whereas 4'-hydroxyaceclofenac was without effect. CONCLUSIONS: These results suggest that aceclofenac actions are multifactorial and that metabolites could contribute to its anti-inflammatory actions. [less ▲]

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See detailEvaluation of classical NSAIDs and COX-2 selective inhibitors on purified ovine enzymes and human whole blood
De Leval, X.; Delarge, J.; Devel, P. et al

in Prostaglandins, Leukotrienes, and Essential Fatty Acids (2001), 64

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See detailPharmacology of the Thromboxane Receptor Antagonist and Thromboxane Synthase Inhibitor Bm-531
Dogné, J. M.; Rolin, S.; de Leval, X. 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 ▲]

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See detailEvaluation de la selectivité COX-1/COX-2 de drogues à visée anti-inflammatoire sur sang humain
De Leval, X.; Delarge, J.; Devel, P. et al

Poster (2000, May)

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