References of "Pirotte, Bernard"
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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 ▲]

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See detailRecent development in the field of dual COX / 5-LOX inhibitors
Julémont, F.; Dogné, J.-M.; Pirotte, Bernard ULg et al

in Mini Reviews in Medicinal Chemistry (2004), 4

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See detailDesign and pharmacological evaluation of recently developed 6-substituted 3-bromophenyl 2-oxo-2H-1-benzopyran 3-carboxylate derivatives as putative inhibitors of cell invasion
Kempen, I.; Frankenne, F.; Telliez, A. et al

in Fundamental & Clinical Pharmacology (2004)

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See detailSynthésis and pharmacological evaluation of original thromboxane A2 receptor antagonists derived from BM-573
Hanson, Julien ULg; Renard, Jean-François ULg; Neven, P. et al

in Fundamental & Clinical Pharmacology (2004)

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See detailNew trends in the design of drugs against Alzheimer's disease
Francotte, Pierre ULg; Graindorge, Emmanuel; Boverie, Stéphane et al

in Current Medicinal Chemistry (2004), 11(13), 1757-1778

First described by Alois Alzheimer in 1907, Alzheimer's disease (AD) is the most common dementia type, affecting approximately 20 million people worldwide. As the population is getting older, AD is a ... [more ▼]

First described by Alois Alzheimer in 1907, Alzheimer's disease (AD) is the most common dementia type, affecting approximately 20 million people worldwide. As the population is getting older, AD is a growing health problem. AD is currently treated by symptomatic drugs, the acetylcholinesterase inhibitors. based on the cholinergic hypothesis (1976). During the past decade, advances in neurobiology have conducted to the identification of new targets. Although some of these innovative approaches tend to delay onset of AD, others are still symptomatic. In this review, we present an overview of the several strategies and new classes of compounds against AD. [less ▲]

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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)

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See detailPharmacological evaluation of BM-573, a dual thromboxane A2 receptor antagonist and thromboxane synthase inhibitor, as potential anti-metastatic agent
De Leval, X.; Dassesse, T.; Benoît, V. et al

Poster (2003, December)

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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)

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See detailEffects of cromakalim analogues on rat pancreatic B-cells, rat aorta rings and rat uterus. Study of their mechanism of action as potassium channel activators
Sebille, S.; Boverie, S.; Becker, B. et al

Poster (2003, November 22)

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See detailPharmacological evaluation of BM-573, a dual thromboxane A(2) receptor antagonist and thromboxane synthase inhibitor, as potential anti-metastatic agent
de Leval, X. J.; Dassesse, T.; Benoit, V. et al

in Blood (2003, November 16), 102(11, Part 2), 72

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See detailTowards tissue-selective KATP channel openers
Lebrun, P.; Antoine, M. H.; Dabrowski, M. et al

Poster (2003, July)

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See detailSynthèse et évaluation pharmacologique de N-pyridinyl-alkanesulfonamides apparentés au nimésulide
Julemont, F.; De Leval, X.; Michaux, C. et al

Poster (2003, May)

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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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