Ambrisentan, a Non-peptide Endothelin Receptor Antagonist
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چکیده
منابع مشابه
Asymmetric synthesis of a selective endothelin A receptor antagonist.
An asymmetric synthesis of a selective endothelin A receptor antagonist 1b is described. Asymmetric conjugate addition of aryllithium derived from 18 to the chiral oxazoline 17 followed by hydrolysis afforded 15 in 96% ee via purification as (S)-(-)-1-phenylethylamine salt. Pd(OAc)(2)/dppf (1,1'-bis(diphenylphosphino)ferrocene) catalyzed carbonylation followed by chemoselective addition of aryl...
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An extremely potent and highly specific non-peptide, subnanomolar endothelin (ET) receptor antagonist, SB 209670, has been synthesized and characterized. SB 209670, which was rationally designed using conformational models of ET-1, selectively inhibits binding of 125I-labeled ET-1 to cloned human ET receptor subtypes ETA and ETB (Ki = 0.2 and 18 nM, respectively). SB 209670 produces concentrati...
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THE ability of the liver to recovcr from ischcmia/rcperfusian (I/R) injury depends on the integrity of thc microcirculation. 1 It has been recently reported that endothelin (ET) plays a major role in the regulation of hepatic microcirculation.2 The aim of this study is to determine whether inhibition of the binding of endothelin to its receptors by a non-selective (ET 1\' ET B) receptor antagon...
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Background: Recent researches have provided evidences of the importance of endothelin axis in carcinogenesis. According to our knowledge, no data exists about endothelin A receptor (ETA) expression in dysplastic oral mucosa (DOM). Therefore, the aim of the present study was to evaluate immunohistochemical expression of ETA in DOM. Methods:</strong...
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Background: Heparanase and endothelin-1/endothelin A receptor (ET-1/ETAR) expressions increase in cancer. This condition enhances tumor progression and correlates with poor survival. Limited data are documented regarding the role of heparanase and ET-1/ETAR in epithelial ovarian cancer (EOC). We sought to characterize the correlation between heparanase and ET-1/ETAR in EOC.Methods: Thirty patie...
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ژورنال
عنوان ژورنال: Cardiovascular Drug Reviews
سال: 2006
ISSN: 0897-5957,1527-3466
DOI: 10.1111/j.1527-3466.2006.00063.x