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Chemical Compound Review:

Volibris 2-(4,6-dimethylpyrimidin-2- yl)oxy-3...

Synonyms: Ambrisentan, CHEMBL302753, SureCN138157, CHEBI:205299, nyl-, (S)-, ...

Galié, N. et al., Bolli, M.H. et al., Kirchengast, M., Uhlmann, D. et al., Vatter, H. et al., et al.

Battistini, Berthiaume, Kelland, Webb, Kohan, Bolli, Marfurt, Grisostomi, Boss, Binkert, Hess, Treiber, Thorin, Morrison, Buchmann, Bur, Ramuz, Clozel, Fischli, Weller, Vatter, Zimmermann, Jung, Weyrauch, Lang, Seifert, Uhlmann, Ludwig, Escher, Armann, Gäbel, Teupser, Tannapfel, Hauss, Witzigmann, Channick, Sitbon, Barst, Manes, Rubin, Kirchengast, Vatter, Zimmermann, Weyrauch, Lange, Setzer, Raabe, Seifert, Uhlmann, Gaebel, Armann, Ludwig, Hess, Pietsch, Fiedler, Tannapfel, Hauss, Witzigmann, Galié, Badesch, Oudiz, Simonneau, McGoon, Keogh, Frost, Zwicke, Naeije, Shapiro, Olschewski, Rubin,

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Disease relevance of BSF-208075

Ambrisentan therapy for pulmonary arterial hypertension [1].
METHODS: In this double-blind, dose-ranging study, 64 patients with idiopathic PAH or PAH associated with collagen vascular disease, anorexigen use, or human immunodeficiency virus infection were randomized to receive 1, 2.5, 5, or 10 mg of ambrisentan once daily for 12 weeks followed by 12 weeks of open-label ambrisentan [1].
CONCLUSIONS: Treatment with the selective ET(A)-RA BSF 208075 has protective effects on microcirculation after 120 min liver ischemia and reperfusion [2].
Furthermore, the pharmacological profile of ambrisentan indicates that this drug may also be suitable in the treatment of cerebrovascular disorders [3].
Protective effect of a selective endothelin a receptor antagonist (BSF 208075) on graft pancreatitis in pig pancreas transplantation [4].

Psychiatry related information on BSF-208075

The animals were divided into 2 groups: the control group received saline solution and the therapy group was given the selective ET(A)-RA BSF 208075 [2].

High impact information on BSF-208075

OBJECTIVES: The purpose of this study was to examine the efficacy and safety of four doses of ambrisentan, an oral endothelin type A receptor-selective antagonist, in patients with pulmonary arterial hypertension (PAH) [1].
The selective endothelin receptor-A antagonists sitaxsentan and ambrisentan are currently undergoing investigation [5].
CONCLUSIONS: Treatment with the selective ET(A)-RA BSF 208075 has protective effects on microcirculation after liver transplantation [6].
The aim of the study was to investigate in vitro the inhibitory effect of LU 208075 on ET-1 and bigET-1 induced contraction and relaxation in rat basilar artery segments [7].
Effect of the novel endothelin(A) receptor antagonist LU 208075 on contraction and relaxation of isolated rat basilar artery [7].

Chemical compound and disease context of BSF-208075

While several compounds, e.g., ambrisentan 2, are in late clinical trials for various indications, one compound (bosentan, Tracleer) is being marketed to treat pulmonary arterial hypertension [8].

Anatomical context of BSF-208075

From the 30 surviving animals coronary arteries were sampled after 6 weeks of oral treatment with 10 mg/kg/day BSF 208075 or vehicle and histologically evaluated [9].

Associations of BSF-208075 with other chemical compounds

In addition, more selective ET(A) receptor antagonists (ambrisentan, atrasentan, avosentan, clazosentan, darusentan, and sitaxsentan) are undergoing clinical trials [10].

Gene context of BSF-208075

The E(max) values for bigET-1 but not for ET-1 were reduced significantly in the presence of LU 208075 [11].
Cerebrovascular characterization of the novel nonpeptide endothelin-A receptor antagonist LU 208075 [11].

Analytical, diagnostic and therapeutic context of BSF-208075

In this animal model, the efficacy of the benzo[e][1,4]diazepin-2-one derivative rac-39au was superior to that of racemic ambrisentan, rac-2 [8].
After pigs underwent coronary artery catheterization they were randomly allocated either to controls or to treatment with the ET receptor antagonist BSF 208075 [9].

References

Ambrisentan therapy for pulmonary arterial hypertension. Galié, N., Badesch, D., Oudiz, R., Simonneau, G., McGoon, M.D., Keogh, A.M., Frost, A.E., Zwicke, D., Naeije, R., Shapiro, S., Olschewski, H., Rubin, L.J. J. Am. Coll. Cardiol. (2005) [Pubmed]
Effects of ET(A) receptor antagonism on proinflammatory gene expression and microcirculation following hepatic ischemia/reperfusion. Uhlmann, D., Gäbel, G., Ludwig, S., Armann, B., Hess, J., Pietsch, U.C., Tannapfel, A., Fiedler, M., Kratzsch, J., Hass, J., Witzigmann, H. Microcirculation (New York, N.Y. : 1994) (2005) [Pubmed]
Ambrisentan, a non-peptide endothelin receptor antagonist. Vatter, H., Seifert, V. Cardiovascular drug reviews. (2006) [Pubmed]
Protective effect of a selective endothelin a receptor antagonist (BSF 208075) on graft pancreatitis in pig pancreas transplantation. Uhlmann, D., Ludwig, S., Escher, E., Armann, B., Gäbel, G., Teupser, D., Tannapfel, A., Hauss, J., Witzigmann, H. Transplant. Proc. (2001) [Pubmed]
Endothelin receptor antagonists in pulmonary arterial hypertension. Channick, R.N., Sitbon, O., Barst, R.J., Manes, A., Rubin, L.J. J. Am. Coll. Cardiol. (2004) [Pubmed]
Attenuation of proinflammatory gene expression and microcirculatory disturbances by endothelin A receptor blockade after orthotopic liver transplantation in pigs. Uhlmann, D., Gaebel, G., Armann, B., Ludwig, S., Hess, J., Pietsch, U.C., Fiedler, M., Tannapfel, A., Hauss, J., Witzigmann, H. Surgery (2006) [Pubmed]
Effect of the novel endothelin(A) receptor antagonist LU 208075 on contraction and relaxation of isolated rat basilar artery. Vatter, H., Zimmermann, M., Jung, C., Weyrauch, E., Lang, J., Seifert, V. Clin. Sci. (2002) [Pubmed]
Novel benzo[1,4]diazepin-2-one derivatives as endothelin receptor antagonists. Bolli, M.H., Marfurt, J., Grisostomi, C., Boss, C., Binkert, C., Hess, P., Treiber, A., Thorin, E., Morrison, K., Buchmann, S., Bur, D., Ramuz, H., Clozel, M., Fischli, W., Weller, T. J. Med. Chem. (2004) [Pubmed]
Endothelin receptor blockade and in-stent restenosis. Kirchengast, M. J. Cardiovasc. Pharmacol. (2001) [Pubmed]
Profile of past and current clinical trials involving endothelin receptor antagonists: the novel "-sentan" class of drug. Battistini, B., Berthiaume, N., Kelland, N.F., Webb, D.J., Kohan, D.E. Exp. Biol. Med. (Maywood) (2006) [Pubmed]
Cerebrovascular characterization of the novel nonpeptide endothelin-A receptor antagonist LU 208075. Vatter, H., Zimmermann, M., Weyrauch, E., Lange, B.N., Setzer, M., Raabe, A., Seifert, V. Clinical neuropharmacology. (2003) [Pubmed]

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