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Bernard Lambermont - One of the best experts on this subject based on the ideXlab platform.
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pharmacological 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 bleedin
Journal of Pharmacology and Experimental Therapeutics, 2004Co-Authors: Jean-michel Dogné, Julien Hanson, Laurence De Leval, Stephanie Rolin, Xavier De Leval, Philippe Kolh, Vincent Tchanasato, Alexandre Ghuysen, Patrick Segers, Bernard LambermontAbstract: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 F2)-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.
Jean-michel Dogné - One of the best experts on this subject based on the ideXlab platform.
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pharmacological 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 bleedin
Journal of Pharmacology and Experimental Therapeutics, 2004Co-Authors: Jean-michel Dogné, Julien Hanson, Laurence De Leval, Stephanie Rolin, Xavier De Leval, Philippe Kolh, Vincent Tchanasato, Alexandre Ghuysen, Patrick Segers, Bernard LambermontAbstract: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 F2)-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.
Laurence De Leval - One of the best experts on this subject based on the ideXlab platform.
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pharmacological 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 bleedin
Journal of Pharmacology and Experimental Therapeutics, 2004Co-Authors: Jean-michel Dogné, Julien Hanson, Laurence De Leval, Stephanie Rolin, Xavier De Leval, Philippe Kolh, Vincent Tchanasato, Alexandre Ghuysen, Patrick Segers, Bernard LambermontAbstract: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 F2)-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.
Patrick Segers - One of the best experts on this subject based on the ideXlab platform.
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pharmacological 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 bleedin
Journal of Pharmacology and Experimental Therapeutics, 2004Co-Authors: Jean-michel Dogné, Julien Hanson, Laurence De Leval, Stephanie Rolin, Xavier De Leval, Philippe Kolh, Vincent Tchanasato, Alexandre Ghuysen, Patrick Segers, Bernard LambermontAbstract: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 F2)-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.
Alexandre Ghuysen - One of the best experts on this subject based on the ideXlab platform.
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pharmacological 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 bleedin
Journal of Pharmacology and Experimental Therapeutics, 2004Co-Authors: Jean-michel Dogné, Julien Hanson, Laurence De Leval, Stephanie Rolin, Xavier De Leval, Philippe Kolh, Vincent Tchanasato, Alexandre Ghuysen, Patrick Segers, Bernard LambermontAbstract: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 F2)-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.