References of "Masereel, B"
     in
Bookmark and Share    
Peer Reviewed
See detailIs thrombin generation the new rapid, reliable and relevant pharmacological tool for the development of anticoagulant drugs?
Robert, S.; Ghiotto, J.; Pirotte, Bernard ULg et al

Conference (2009, November)

Detailed reference viewed: 19 (1 ULg)
Full Text
Peer Reviewed
See detailIs thrombin generation the new rapid, reliable and relevant pharmacological tool for the development of anticoagulant drugs ?
Robert, S.; Ghiotto, J.; Pirotte, Bernard ULg et al

in Pharmacological Research (2009), 59

Detailed reference viewed: 16 (3 ULg)
Full Text
Peer Reviewed
See detailSynthesis and pharmacological evaluation of a new targeted drug carrier system: β-Cyclodextrin coupled to oxytocin
Bertolla, C; Rolin, S; Evrard, Brigitte ULg et al

in Bioorganic & Medicinal Chemistry Letters (2008), 18

β-Cyclodextrin (β-CD) was monofunctionalized into its carboxylic derivative and then conjugated to the N-side of oxytocin (OT), a nonapeptide involved in human behavior and myometrium contraction. On ... [more ▼]

β-Cyclodextrin (β-CD) was monofunctionalized into its carboxylic derivative and then conjugated to the N-side of oxytocin (OT), a nonapeptide involved in human behavior and myometrium contraction. On isolated rat myometrium, this conjugate (β-CD-OT) partly preserves the contracting activity of OT (EC50 = 0.40 μM vs 1.7 nM). Moreover, the contraction induced frequency is also lowered by β-CD-OT. This novel hydrophilic targeted carrier could form a host–guest complex with prostaglandins and their derivatives used as labor inducers or with anticancer drugs used in cervix and endometrial cancer. This strategy can improve the solubility, the stability, and/or the biological activity of these drugs as well as reducing their side-effects. [less ▲]

Detailed reference viewed: 13 (2 ULg)
Peer Reviewed
See detailThrombin activity profile: a rapid, reliable and relevant ex vivo screening test for the development of anticoagulant drugs
Robert, S.; Ghiotto, J.; Pirotte, Bernard ULg et al

Conference (2007, October)

Detailed reference viewed: 7 (0 ULg)
Peer Reviewed
See detailThrombin activity profile : a powerful ex vivo screening test for the development of anticoagulant drugs
Robert, S.; Ghiotto, J.; Pirotte, Bernard ULg et al

Poster (2007, July)

Detailed reference viewed: 8 (0 ULg)
Full Text
Peer Reviewed
See detailBM-520, an original TXA(2) modulator, inhibits the action of thromboxane A(2) and 8-iso-prostaglandin F-2 alpha in vitro and in vivo on human and rodent platelets, and aortic vascular smooth muscles from rodents
Rolin, S.; Hanson, Julien ULg; Vastersaegher, C. et al

in Prostaglandins & Other Lipid Mediators (2007), 84(1-2), 14-23

Thromboxane A(2) (TXA(2)) and 8-iso-PGF(2 alpha). are two prostanoid agonists of the thromboxane A(2) receptor (TP), whose activation has been involved in platelet aggregation and atherosclerosis. Agents ... [more ▼]

Thromboxane A(2) (TXA(2)) and 8-iso-PGF(2 alpha). are two prostanoid agonists of the thromboxane A(2) receptor (TP), whose activation has been involved in platelet aggregation and atherosclerosis. Agents able to counteract the actions of these agonists are of great interest in the treatment and prevention of cardiovascular events. Here, we investigated in vitro and in vivo the pharmacological profile of BM-520, a new TP antagonist. In our experiments, this compound showed a great binding affinity for human washed platelets TP receptors, and prevented human platelet activation and aggregation induced by U-46619, arachidonic acid and 8-iso-PGF(2 alpha). The TP receptor antagonist property of BM-520 was confirmed by its relaxing effect on rat aorta smooth muscle preparations precontracted with U-46619 and 8-iso-PGF(2 alpha). Further, its TP antagonism was also demonstrated in vivo in guinea pig after a single intravenous injection (10 mg kg(-1)). We conclude that this novel TP antagonist could be a promising therapeutic tool in pathologies such as atherosclerosis where an increased production of TXA(2) and 8-iso-PGF2., as well as TP activation are well-established pathogenic events. (c) 2007 Elsevier Inc. All rights reserved. [less ▲]

Detailed reference viewed: 15 (2 ULg)
Full Text
Peer Reviewed
See detailEvaluation of BM-573, a novel TXA(2) synthase inhibitor and receptor antagonist, in a porcine model of myocardial ischemia-reperfusion
Kolh, Philippe ULg; Rolin, S.; Tchana-Sato, Vincent ULg et al

in Prostaglandins & Other Lipid Mediators (2006), 79(1-2), 53-73

Aims: To investigate whether BM-573 (N-tert-butyl-N'-[2-(4'-methylphenylam\ino)-5-nitro-benzenesulfonyl]urea), an original combined thromboxane A(2) synthase inhibitor and receptor antagonist, prevents ... [more ▼]

Aims: To investigate whether BM-573 (N-tert-butyl-N'-[2-(4'-methylphenylam\ino)-5-nitro-benzenesulfonyl]urea), an original combined thromboxane A(2) synthase inhibitor and receptor antagonist, prevents reperfusion injury in acutely ischemic pigs. Methods: Twelve animals were randomly divided in two groups: a control group (n = 6) intravenously infused with vehicle, and a BM-573-treated group (n = 6) infused with BM-573 (10 mg kg(-1) h(-1)). In both groups, the left anterior descending (LAD) coronary artery was Occluded for 60 min and reperfused for 240 min. Either vehicle or BM-573 was infused 30 min before LAD occlusion and throughout the experiment. Platelet aggregation induced by arachidonic acid ex vivo measured was prevented by BM-573. Results: In both groups, LAD occlusion decreased cardiac output, ejection fraction, slope of stroke work-end-diastolic volume relationship, and induced end-systolic pressure-volume relationship (ESPVR) rightward shift, while left ventricular afterload increased. Ventriculo-arterial coupling and mechanical efficiency decreased. In both groups, reperfusion further decreased cardiac output and ejection fraction, while ESPVR displayed a further rightward shift. Ventriculo-arterial coupling and mechanical efficiency remained impaired. Area at risk, evidenced with Evans blue, was 33.2 +/- 3.4% of the LV mass (LVM) in both groups, and mean infarct size, revealed by triphenyltetrazolium chloride (TTC), was 27.3 +/- 2.6% of the LVM in the BM-573-treated group (NS). Histological examination and immunohistochemical identification of desmin revealed necrosis in the anteroseptal region similar in both groups, while myocardial ATP dosages and electron microscopy also showed that BM-573 had no cardioprotective effect. Conclusions: These data suggest that BM-573 failed to prevent reperfusion injury in acutely ischemic pigs. (C) 2005 Elsevier Inc. All rights reserved. [less ▲]

Detailed reference viewed: 40 (10 ULg)
Full Text
Peer Reviewed
See detail3,6-Disubstitued coumarins as mechanism-based inhibitors of thrombin and factor Xa
Frederick, R.; Robert, S.; Charlier, C. et al

in Journal of Medicinal Chemistry (2005), 48

Detailed reference viewed: 10 (4 ULg)
Full Text
Peer Reviewed
See detailEffect of a novel thromboxane A(2) inhibitor on right ventricular-arterial coupling in endotoxic shock
Lambermont, Bernard ULg; Kolh, Philippe ULg; Ghuysen, Alexandre ULg et al

in Shock (2004), 21(1), 45-51

We investigated the effects of a dual thromboxane (TX)A(2) synthase inhibitor and TXA(2) receptor antagonist (BM-573) on right ventricular-arterial coupling in a porcine model of endotoxic shock. Thirty ... [more ▼]

We investigated the effects of a dual thromboxane (TX)A(2) synthase inhibitor and TXA(2) receptor antagonist (BM-573) on right ventricular-arterial coupling in a porcine model of endotoxic shock. Thirty minutes before the onset of 0.5 mg/kg endotoxin infusion, six pigs (Endo group) received an infusion with a placebo solution, and six other pigs (Anta group) with BM-573. Right ventricular pressure-volume loops were obtained by the conductance catheter technique. The slope (E-es) of the end-systolic pressure-volume relationship and its volume intercept at 25 mmHg were calculated as measures of right ventricular systolic function. RV afterload was quantified by pulmonary arterial elastance (E-a), and E-es/E-a ratio represented right ventricular-arterial coupling. Mechanical efficiency was defined as the ratio of stroke work and pressure-volume area. In this model of endotoxic shock, BM-573 blunted the early phase of pulmonary hypertension, improved arterial oxygenation, and prevented a decrease in right ventricular myocardial efficiency and right ventricular dilatation. However, the drug could not prevent the loss of homeometric regulation and alterations in right ventricular-arterial coupling. In conclusion, dual TXA(2) synthase inhibitor and receptor antagonists such as BM-573 have potential therapeutic applications, improving right ventricular efficiency and arterial oxygenation in endotoxic shock. [less ▲]

Detailed reference viewed: 24 (2 ULg)
Full Text
Peer Reviewed
See detailNew developments on thromboxane modulators
Dogné, Jean-Michel ULg; Hanson, Julien ULg; De leval, X. et al

in Mini Reviews in Medicinal Chemistry (2004)

Detailed reference viewed: 19 (3 ULg)
Full Text
Peer Reviewed
See detailNew developments on thromboxane and prostacyclin modulators. Part II: prostacyclin modulators
De Leval, X.; Hanson, Julien ULg; David, Jean-Louis ULg et al

in Current Medicinal Chemistry (2004), 11

Detailed reference viewed: 21 (1 ULg)
Full Text
Peer Reviewed
See detailCharacterization of preferential activity on platelet thromboxane A2 receptors of BM-613, a new thromboxane A2 antagonist
Hanson, Julien ULg; Rolin, S.; De Leval, X. et al

in Fundamental & Clinical Pharmacology (2004)

Detailed reference viewed: 3 (1 ULg)
Full Text
Peer Reviewed
See detailNew developments on thromboxane and prostacyclin modulators. Part I: thromboxane modulators
Dogné, Jean-Michel ULg; De leval, X.; Hanson, Julien ULg et al

in Current Medicinal Chemistry (2004), 11

Detailed reference viewed: 21 (2 ULg)
Full Text
Peer Reviewed
See detailPharmacological characterization of N-tert-butyl-N’-[2-(4’-methylphenylamino)-5-nitrobenzenesulfonyl]urea (BM-573), a novel thromboxane A2 receptor antagonist and thromboxane synthase inhibitor in a rat model of arterial thrombosis and its effects on bleeding time
Dogné, Jean-Michel ULg; Hanson, Julien ULg; De leval, X. et al

in Journal of Pharmacology and Experimental Therapeutics (The) (2004), 309(2), 498-505

The present study was undertaken to characterize the antiplatelet and antithrombotic effects of BM-573 [N-tert-butyl-N'-[2-(4'-methylphenylamino)-5-nitrobenzenesulfonyl] urea], an original combined ... [more ▼]

The present study was undertaken to characterize the antiplatelet and antithrombotic effects of BM-573 [N-tert-butyl-N'-[2-(4'-methylphenylamino)-5-nitrobenzenesulfonyl] urea], an original combined thromboxane receptor antagonist and thromboxane synthase inhibitor in rats, and to determine its effects on mice bleeding time. Intraperitoneal injection of a single dose of 5 mg/kg BM-573 to rats inhibited U-46619 (9,11-dideoxy-9,11-methanoepoxy-prostaglandin F-2)-induced washed platelet aggregation 30 min and 1, 2, and 4 h after drug administration with a maximum antiplatelet effect observed after 1 and 2 h. In a rat model of thrombosis induced by ferric chloride application on the abdominal aorta, BM-573 significantly reduced the thrombus weight by 92.53, 80.20, 64.75, and 18.21% at doses of 5, 2, 0.5, and 0.2 mg/kg, respectively. Time to occlusion of abdominal aorta in the BM-573-treated group (41.50+/-5.21 min) was significantly prolonged compared with the vehicle-treated rats (16.16+/-0.79 min). Like furegrelate, seratrodast, and acetylsalicylic acid, BM-573 did not affect the tail bleeding time induced by tail transection in mice compared with vehicle-treated mice. Moreover, BM-573, a close derivative of the loop diuretic torasemide, failed to induce a significant increase in diuresis in rat and did not produce a decrease in blood glucose concentration as observed with the sulfonylurea glibenclamide. In conclusion, we have demonstrated that the nitrobenzenic sulfonylurea BM-573, an original combined thromboxane receptor antagonist and thromboxane synthase inhibitor, is a potent antithrombotic agent that does not affect bleeding time. Moreover, BM-573 lost the diuretic property of torasemide and has no impact on glycemia. [less ▲]

Detailed reference viewed: 57 (16 ULg)
Peer Reviewed
See detailBM-613, a new thromboxane A2 antagonist, is characterized by a preferential activity on platelet thromboxane A2 receptors
Hanson, Julien ULg; Rolin, S.; De Leval, X. et al

Poster (2003, December)

Detailed reference viewed: 8 (0 ULg)
Peer Reviewed
See detailBM-613, a new thromboxane A2 antagonist, is characterized by a preferential activity on platelet thromboxane A2 receptors
Hanson, Julien ULg; Rolin, S.; De Leval, X. et al

Poster (2003, November 22)

Detailed reference viewed: 3 (1 ULg)