Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

Editor

Personal info

View

About

Terms

Javascript disabled

Please enable Javascript support in your browser to use this application.

Instructions on how to enable JavaScript on different browsers can be found here: http://www.google.com/support/bin/answer.py?answer=23852.

[edit this page]

Chemical Compound Review:

CHEMBL210602 3-[2-[(4-methylphenyl)amino]- 5-nitro...

Synonyms: BM-573, SureCN3393325, CHEBI:449741, NSC-732094, AC1NSM3C, ...

Rolin, S. et al., Kolh, P. et al., Tchana-Sato, V. et al., Dogné, J.M. et al., Ghuysen, A. et al., et al.

Dogné, Hanson, de Leval, Kolh, Tchana-Sato, de Leval, Rolin, Ghuysen, Segers, Lambermont, Masereel, Pirotte, Kolh, Rolin, Tchana-Sato, Pétein, Ghuysen, Lambermont, Hanson, Magis, Segers, Masereel, D'Orio, Dogne, Lambermont, Kolh, Ghuysen, Segers, Dogné, Tchana-Sato, Morimont, Benoit, Gérard, Masereel, D'Orio, Tchana-Sato, Dogné, Lambermont, Ghuysen, Magis, Morimont, Hanson, D'Orio, Limet, Kolh, Ghuysen, Dogné, Chiap, Rolin, Masereel, Lambermont, Kolh, Tchana-Sato, Hanson, D'Orio, de Leval, Dassesse, Dogné, Waltregny, Bellahcène, Benoit, Pirotte, Castronovo, Ghuysen, Lambermont, Dogné, Kolh, Tchana-Sato, Morimont, Magis, Hanson, Segers, D'Orio,

Welcome! If you are familiar with the subject of this article, you can contribute to this open access knowledge base by deleting incorrect information, restructuring or completely rewriting any text. Read more.

Disease relevance of BM-573

These data suggest that BM-573 could be useful for the prevention of myocardial infarction [1].
Among the BM-573-treated group, four pigs did not develop coronary artery thrombus and their myocardium appeared healthy [1].
The aim of this study was to evaluate the effect of BM-573 [N-terbutyl-N'-[2-(4'-methylphenylamino)-5-nitro-benzenesulfonyl]urea], a dual thromboxane A2 synthase inhibitor and receptor antagonist, on the hemodynamic response to acute pulmonary embolism [2].
In conclusion, dual TXA2 synthase inhibitor and receptor antagonists such as BM-573 have potential therapeutic applications, improving right ventricular efficiency and arterial oxygenation in endotoxic shock [3].
Moreover, BM-573 significantly decreased early atherogenesis and prevented progression of established atherosclerotic lesions [4].

High impact information on BM-573

The highest rates of cell migration inhibition were obtained with original compounds BM-567 and BM-573 (50.3 and 59.4% inhibition, respectively) when used at the final concentration of 10 microM [5].
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) [6].
We conclude that in this animal model of acute pulmonary embolism, infusion of BM-573 reduced pulmonary vasoconstriction [2].
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 [6].
Histopathological examination of FeCl3-injured coronary artery revealed an occlusive and adherent thrombus in control group, while pretreatment with BM-573 prevented thrombus formation [1].

Chemical compound and disease context of BM-573

In both treatments, while BM-573 did not affect body weight, systolic blood pressure, total plasma cholesterol or triglycerides levels, it partially reduced TxA(2) but did not affect prostacyclin biosynthesis [4].
In vivo, BM-573 appears to have antiplatelet and antithrombotic activities since it reduced thrombus weight and prolonged the time to abdominal aorta occlusion induced by ferric chloride [7].

Biological context of BM-573

In the same conditions, BM-573 completely blocked the increase of arterial elastance, and stabilized both mean aortic blood pressure and mean systemic blood flow [8].
The effects of each dose of BM-573 on ex vivo platelet aggregation induced by arachidonic acid, collagen or ADP were also evaluated [8].
These results suggest that BM-573 should be viewed as a promising therapeutic agent in the treatment of pulmonary hypertension and syndromes associated with platelet activation [7].
In conclusion, BM-573 could therefore be a promising therapeutic approach in pathophysiological states where TXA2 plays a main role in the increase of vascular resistance like in pathologies such as systemic hypertension [8].

Anatomical context of BM-573

BM-573 relaxed the isolated rat thoracic aorta (ED(50)=28.4 nM) and guinea-pig trachea (ED(50)=17.7 nM) contracted by U-46619 [9].

Associations of BM-573 with other chemical compounds

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) [10].

Gene context of BM-573

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 [10].

Analytical, diagnostic and therapeutic context of BM-573

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 [1].
CONCLUSIONS: These data suggest that BM-573 failed to prevent reperfusion injury in acutely ischemic pigs [10].

References

BM-573, a dual thromboxane synthase inhibitor and thromboxane receptor antagonist, prevents pig myocardial infarction induced by coronary thrombosis. Rolin, S., Petein, M., Tchana-Sato, V., Dogne, J.M., Benoit, P., Lambermont, B., Ghuysen, A., Kolh, P., Masereel, B. J. Pharmacol. Exp. Ther. (2003) [Pubmed]
Effect of BM-573 [N-terbutyl-N'-[2-(4'-methylphenylamino)-5-nitro-benzenesulfonyl]urea], a dual thromboxane synthase inhibitor and thromboxane receptor antagonist, in a porcine model of acute pulmonary embolism. Ghuysen, A., Lambermont, B., Dogné, J.M., Kolh, P., Tchana-Sato, V., Morimont, P., Magis, D., Hanson, J., Segers, P., D'Orio, V. J. Pharmacol. Exp. Ther. (2004) [Pubmed]
Effect of a novel thromboxane A2 inhibitor on right ventricular-arterial coupling in endotoxic shock. Lambermont, B., Kolh, P., Ghuysen, A., Segers, P., Dogné, J.M., Tchana-Sato, V., Morimont, P., Benoit, P., Gérard, P., Masereel, B., D'Orio, V. Shock (2004) [Pubmed]
A novel thromboxane receptor antagonist and synthase inhibitor, BM-573, reduces development and progression of atherosclerosis in LDL receptor deficient mice. Cyrus, T., Yao, Y., Ding, T., Dogné, J.M., Praticò, D. Eur. J. Pharmacol. (2007) [Pubmed]
Evaluation of original dual thromboxane A2 modulators as antiangiogenic agents. de Leval, X., Dassesse, T., Dogné, J.M., Waltregny, D., Bellahcène, A., Benoit, V., Pirotte, B., Castronovo, V. J. Pharmacol. Exp. Ther. (2006) [Pubmed]
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 bleeding time. Dogné, J.M., Hanson, J., de Leval, X., Kolh, P., Tchana-Sato, V., de Leval, L., Rolin, S., Ghuysen, A., Segers, P., Lambermont, B., Masereel, B., Pirotte, B. J. Pharmacol. Exp. Ther. (2004) [Pubmed]
Pharmacological profile and therapeutic potential of BM-573, a combined thromboxane receptor antagonist and synthase inhibitor. Ghuysen, A., Dogné, J.M., Chiap, P., Rolin, S., Masereel, B., Lambermont, B., Kolh, P., Tchana-Sato, V., Hanson, J., D'Orio, V. Cardiovascular drug reviews. (2005) [Pubmed]
Effects of BM-573, a thromboxane A2 modulator on systemic hemodynamics perturbations induced by U-46619 in the pig. Tchana-Sato, V., Dogné, J.M., Lambermont, B., Ghuysen, A., Magis, D., Morimont, P., Hanson, J., D'Orio, V., Limet, R., Kolh, P. Prostaglandins Other Lipid Mediat. (2005) [Pubmed]
Activity of a novel dual thromboxane A(2)receptor antagonist and thromboxane synthase inhibitor (BM-573) on platelet function and isolated smooth muscles. Rolin, S., Dogné, J.M., Michaux, C., Delarge, J., Masereel, B. Prostaglandins Leukot. Essent. Fatty Acids (2001) [Pubmed]
Evaluation of BM-573, a novel TXA2 synthase inhibitor and receptor antagonist, in a porcine model of myocardial ischemia-reperfusion. Kolh, P., Rolin, S., Tchana-Sato, V., Pétein, M., Ghuysen, A., Lambermont, B., Hanson, J., Magis, D., Segers, P., Masereel, B., D'Orio, V., Dogne, J.M. Prostaglandins Other Lipid Mediat. (2006) [Pubmed]

Contributions to this collaborative article are from individual authors of WikiGenes or mined by the WikiGenes Data Mining Engine from MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.About WikiGenes Open Access Licence Privacy Policy Terms of Use apsburg

The world's first wiki where authorship really matters (Nature Genetics, 2008). Due credit and reputation for authors. Imagine a global collaborative knowledge base for original thoughts. Search thousands of articles and collaborate with scientists around the globe.