References of "Masereel, B."
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See detailEffects of endotoxic shock on right ventricular systolic function and mechanical efficiency
Lambermont, Bernard ULg; Ghuysen, Alexandre ULg; Kolh, Philippe ULg et al

in Cardiovascular Research (2003), 59(2), 412-418

Objective: To investigate the effects of endotoxin infusion on right ventricular (RV) systolic function and mechanical efficiency. Methods: Six anesthetized pigs (Endo group) received a 0.5 mg/kg ... [more ▼]

Objective: To investigate the effects of endotoxin infusion on right ventricular (RV) systolic function and mechanical efficiency. Methods: Six anesthetized pigs (Endo group) received a 0.5 mg/kg endotoxin infusion over 30 min and were compared with six other anesthetized pigs (Control group) receiving placebo for 5 h. RV pressure-volume (PV) loops were obtained by the conductance catheter technique and pulmonary artery flow and pressure were measured with high-fidelity transducers. Results: RV adaptation to increased afterload during the early phase of endotoxin-induced pulmonary hypertension (T30) was obtained by both homeometric and hetereometric regulations: the slope of the end-systolic PV relationship of the right ventricle increased from 1.4+/-0.2 mmHg/ml to 2.9+/-0.4 mmHg/ml (P<0.05) and RV end-diastolic volume increased from 56+/-6 ml to 64+/-11 ml (P<0.05). Consequently, right ventricular-vascular coupling was maintained at a maximum efficiency. Ninety minutes later (T120), facing the same increased afterload, the right ventricle failed to maintain its contractility to such an elevated level and, as a consequence, right ventricular-vascular uncoupling occurred. PV loop area, which is known to be highly correlated with oxygen myocardial consumption, increased from 1154+/-127 mmHg/ml (T0) to 1798+/-122 mmHg/ml (T180) (P<0.05) while RV mechanical efficiency decreased from 63+/-2% (T0) to 45+/-5% (T270) (P<0.05). Conclusions: In the very early phase of endotoxinic shock, right ventricular-vascular coupling is preserved by an increase in RV contractility. Later, myocardial oxygen consumption and energetic cost of RV contractility are increased, as evidenced by the decrease in RV efficiency, and right ventricular-vascular uncoupling occurs. Therefore, therapies aiming at restoring right ventricular-vascular coupling in endotoxic shock should attempt to increase RV contractility and to decrease RV afterload but also to preserve RV mechanical efficiency. (C) 2003 European Society of Cardiology. Published by Elsevier B.V. All rights reserved. [less ▲]

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See detailBM-573, a dual thromboxane synthase inhibitor and thromboxane receptor antagonist, prevents pig myocardial infarction induced by coronary thrombosis
Rolin, S.; Petein, M.; Tchana-Sato, Vincent ULg et al

in Journal of Pharmacology and Experimental therapeutics (2003), 306(1), 59-65

The aim of this study was to characterize the effects of BM-573 [N-terbutyl-N'-[2-(4'-methylphenylamino)-5-nitro-benzenesulfonyl] urea], a novel dual thromboxane A 2 receptor antagonist and thromboxane ... [more ▼]

The aim of this study was to characterize the effects of BM-573 [N-terbutyl-N'-[2-(4'-methylphenylamino)-5-nitro-benzenesulfonyl] urea], a novel dual thromboxane A 2 receptor antagonist and thromboxane synthase inhibitor, on myocardial infarction induced by topical ferric chloride (FeCl3) application to the left anterior descending (LAD) coronary artery in anesthetized pigs. All control animals (n = 6) developed an occlusive thrombus in the LAD coronary artery. The mean infarct size, revealed by triphenyl tetrazolium chloride (TTC), and the area at risk, evidenced by Evans blue, corresponded to 35.3 +/- 2.2 and 36.9 +/- 2.1% of the left ventricular mass, respectively. In the BM-573-treated group (n = 6), a drug infusion (10 mg . kg(-1) . h(-1)) started 30 min before FeCl3 application and continued throughout the experimentation. Among the BM-573-treated group, four pigs did not develop coronary artery thrombus and their myocardium appeared healthy. Histopathological examination of FeCl3-injured coronary artery revealed an occlusive and adherent thrombus in control group, while pretreatment with BM-573 prevented thrombus formation. In infarcted zones, lack of desmin staining and muscle structure disorganization were obvious. Depletion of myocardial ATP content was observed in the myocardial necrotic region of the control group, but not in myocardial samples of BM-573-treated pigs that did not develop myocardial infarction. When BM-573 prevented LAD artery occlusion, the area under the curve of plasmatic troponin T was reduced by 77% over 6 h. These data suggest that BM-573 could be useful for the prevention of myocardial infarction. [less ▲]

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See detailEffects of U-46619 on Pulmonary Hemodynamics before and after Administration of Bm-573, a Novel Thromboxane A2 Inhibitor
Lambermont, Bernard ULg; Kolh, Philippe ULg; Dogné, Jean-Michel ULg et al

in Archives of Physiology & Biochemistry (2003), 111(3), 217-23

We studied the effects on pulmonary hemodynamics of U-46619, a thromboxane A2 (TXA2) agonist, before and after administration of a novel TXA2 receptor antagonist and synthase inhibitor (BM-573). Six ... [more ▼]

We studied the effects on pulmonary hemodynamics of U-46619, a thromboxane A2 (TXA2) agonist, before and after administration of a novel TXA2 receptor antagonist and synthase inhibitor (BM-573). Six anesthetized pigs (Ago group) received 6 consecutive injections of U-46619 at 30-min interval and were compared with six anesthetized pigs (Anta group) which received an increasing dosage regimen of BM-573 10 min before each U-46619 injection. Consecutive changes in pulmonary hemodynamics, including characteristic resistance, vascular compliance, and peripheral vascular resistance, were continuously assessed during the experimental protocol using a four-element Windkessel model. At 2 mg/kg, BM-573 completely blocked pulmonary hypertensive effects of U-46619 but pulmonary vascular compliance still decreased. This residual effect can probably be explained by a persistent increase in the tonus of the pulmonary vascular wall smooth muscles sufficient to decrease vascular compliance but not vessel lumen diameter. Such molecule could be a promising therapeutic approach in TXA2 mediated pulmonary hypertension as it is the case in pulmonary embolism, hyperacute lung rejection and endotoxinic shock. [less ▲]

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See detailEffects of Bm-573, a Novel Thromboxane A2 Inhibitor, on Pulmonary Hemodynamics in Endotoxic Shock
Lambermont, Bernard ULg; Ghuysen, Alexandre ULg; Dogné, Jean-Michel ULg et al

in Archives of Physiology & Biochemistry (2003), 111(3), 224-31

Thromboxane A2 is considered to be partially responsible for the increase in pulmonary vascular resistance observed after endotoxin administration and to participate in proinflammatory reactions. The ... [more ▼]

Thromboxane A2 is considered to be partially responsible for the increase in pulmonary vascular resistance observed after endotoxin administration and to participate in proinflammatory reactions. The effects of a novel dual TXA2 synthase inhibitor and TXA2 receptor antagonist (BM-573) on pulmonary hemodynamics were investigated in endotoxic shock. 30 mins before the start of a 0.5 mg/kg endotoxin infusion, 6 pigs (Endo group) received a placebo infusion and 6 other pigs (Anta group) received a BM-573 infusion. In Endo group, pulmonary artery pressure increased from 25 +/- 1.8 (T0) to 42 +/- 2.3 mmHg (T60) (p < 0.05) after endotoxin infusion while, in Anta group, it increased from 23 +/- 1.6 (T0) to 25 +/- 1.5 mmHg (T60). This difference is due to a reduction in pulmonary vascular resistance in Anta group while pulmonary arterial compliance changes in Endo group remained comparable with the evolution in Anta group. In Endo group, PaO2 decreased from 131 +/- 21 (T0) to 74 +/- 12 mmHg (T300) (p < 0.05), while in Anta group, PaO2 was 241 +/- 31 mmHg at the end of the experimental period (T300). These results demonstrate that TXA2 plays a major role in pulmonary vascular changes during endotoxin insult. Concomitant inhibition of TXA2 synthesis and of TXA2 receptors by BM-573 inhibited the pulmonary vasopressive response during the early phase of endotoxin shock as well as the deterioration in arterial oxygenation. [less ▲]

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See detailSynthèse et évaluation biologique de nouvelles coumarines en tant qu’anticoagulants potentiels
Pochet, L.; Rolin, S.; Morel, M. et al

Poster (2003, May)

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See detailPharmacological evaluation of the thromboxane A2 receptor antagonist BM-613
Hanson, Julien ULg; Rolin, S.; De Leval, X. et al

Poster (2003, May)

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See detailSynthesis and pharmacological evaluation of BM-613, an original thromboxane A2 antagonist
Hanson, Julien ULg; Rolin, S.; De Leval, X. et al

Poster (2003, May)

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See detail3-Bromophenyl 6-acetoxymethyl-2-oxo-2H-1-benzopyran-3-carboxylate inhibits cancer cell invasion in vitro and tumour growth in vivo
Kempen, I.; Papapostolou, D.; Thierry, N. et al

in British Journal of Cancer (2003), 88(7), 1111-1118

In search for new anticancer agents, we have evaluated the antiinvasive and antimigrative properties of recently developed synthetic coumarin derivatives among which two compounds revealed important ... [more ▼]

In search for new anticancer agents, we have evaluated the antiinvasive and antimigrative properties of recently developed synthetic coumarin derivatives among which two compounds revealed important activity: 3-chlorophenyl 6-acetoxymethyl-2-oxo-2H-1-benzopyran-3-carboxylate and 3-bromophenyl 6-acetoxymethyl-2-oxo-2H-1-benzopyran-3-carboxylate, Both drugs were able to inhibit cell invasion markedly in a Boyden chamber assay, the bromo derivative being more potent than the reference matrix metalloprotease (MMP) inhibitor GI 129471. In vivo, tumour growth was reduced when nude mice grafted with HT 1080 or MDA-MB231 cells were treated i.p. 3 days week(-1) with the bromo coumarin derivative. These effects were not associated with the inhibition of urokinase, plasmin, MMP-2 or MMP-9. The mechanism of action of the drugs remains to be elucidated. However, these two coumarin derivatives may serve as new lead compounds of an original class of antitumour agents. [less ▲]

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See detailEtude de la sélectivité tissulaire d’un nouvel antagoniste des récepteurs au thromboxane A2, le BM-613
Hanson, Julien ULg; Rolin, S.; De Leval, X. et al

Poster (2003, January 31)

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See detailPharmacological evaluation of the novel thromboxane modulator BM-567 (I/II). Effects of BM-567 on platelet function
Dogne, J. M.; de Leval, X.; Kolh, Philippe ULg et al

in Prostaglandins, Leukotrienes, and Essential Fatty Acids (2003), 68(1), 49-54

The aim of this work was to evaluate the effects of BM-567 ( N-pentyl-N'-[(2-cyclohexylamino-5-nitrobenzene)sulfonyl]urea), a torasemide derivative. on both thromboxane A(2) (TXA(2)) receptors (TP) and ... [more ▼]

The aim of this work was to evaluate the effects of BM-567 ( N-pentyl-N'-[(2-cyclohexylamino-5-nitrobenzene)sulfonyl]urea), a torasemide derivative. on both thromboxane A(2) (TXA(2)) receptors (TP) and thromboxane synthase of human platelets. The drug affinity for TP receptors of human washed platelets has been determined. In this test BM-567 showed a high affinity (IC50: 1.1+/-0.1 nM) for the TP receptors in comparison with BM-531 (IC50: 7.8+/-0.7 nM) and sulotroban (IC50: 931+/-85 nM), two TXA(2) antagonists. We also demonstrated that BM-567 prevented platelet aggregation induced by arachidonic acid (AA) (600 muM) (ED100: 0.20+/-0.10muM), U-46619, a stable TXA(2) agonist (1 muM) (ED50: 0.30+/-0.04 muM) and collagen (1 mug ml(-1)) (% of inhibition: 44.3+/-4.3% at 10 muM) and inhibited the second wave of ADP (2 muM). Moreover, when BM-567 was incubated in whole blood from healthy donors, the closure time measured by the Platelet Function analyzer (PFA-100) was significantly prolonged (closure time: 215+/-21 s) by using collagen/epinephrine cartridges. Finally, at the concentration of 1 muM, BM-567 completely reduced the TXB2 production from human platelets stimulated with AA (600 muM). These results indicate that BM-567 is a novel combined TXA(2) receptor antagonist and thromboxane synthase inhibitor characterized by a powerful antiplatelet potency. (C) 2002 Elsevier Science Ltd. All rights reserved. [less ▲]

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See detailEvaluation of classical NSAIDS on COX-1 and COX-2 purifies enzymes and prognosis of their effects on physiological responses.
De Leval, X.; Henrotin, Yves ULg; Masereel, B. et al

in Fundamental & Clinical Pharmacology (2003), 14

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See detailA dual thromboxane inhibitor and thromboxane receptor antagonist prevents pig myocardial infarction induced by coronary thrombosis
Rolin, S.; Petein, M.; Tchana-Sato, Vincent ULg et al

in European Heart Journal (2003), 24(Suppl. S), 325

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See detailInvestigation of the inhibition mechanism of coumarins on chymotrypsin by mass spectrometry
Pochet, L.; Dieu, M.; Frederick, R. et al

in Tetrahedron (2003)

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See detailPharmacological evaluation of the novel thromboxane modulator BM-567 (II/II). Effects of BM-567 on osteogenic sarcoma-cell-induced platelet aggregation
De Leval, X.; Benoit, V.; Delarge, J. et al

in Prostaglandins, Leukotrienes, and Essential Fatty Acids (2003)

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See detailPharmacological evaluation of the novel thromboxane modulator BM-567 (I/II). Effects of BM-567 on platelet function
Dogné, Jean-Michel ULg; De Leval, X.; Kolh, Philippe ULg et al

in Prostaglandins, Leukotrienes, and Essential Fatty Acids (2003)

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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.; Benoît, V.; Neven, P. et al

Poster (2002, October)

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