Atrasentan has also been used to treat cardiovascular disease.[1]
Biochem/physiol Actions
Atrasentan is a selective endothelin ETA receptor antagonist with an IC50 of 0.2 nM for ETA compared to 190 nM for ETB receptors. It blocks blocks endothelin induced cell proliferation, and has been investigated as a possible treatment for prostate cancer, and more recently for therapy for diabetic kidney disease.
Atrasentan, a selective endothelin A receptor antagonist, has been shown to reduce albuminuria in type 2 diabetes. We previously showed that the structural integrity of a glomerular endothelial glycocalyx is required to prevent albuminuria. Therefore we tested the potential of
Determination of atrasentan by high performance liquid chromatography with fluorescence detection in human plasma.
Endothelin-1 (ET-1) promotes renal damage during cardiovascular disease; yet, the molecular mechanisms involved remain unknown. Endoplasmic reticulum (ER) stress, triggered by unfolded protein accumulation in the ER, contributes to apoptosis and organ injury. These studies aimed to determine whether the
The Journal of pharmacology and experimental therapeutics, 351(2), 467-473 (2014-09-06)
Experiments determined whether the combination of endothelin A (ETA) receptor antagonist [ABT-627, atrasentan; (2R,3R,4S)-4-(1,3-benzodioxol-5-yl)-1-[2-(dibutylamino)-2-oxoethyl]-2-(4-methoxyphenyl)pyrrolidine-3-carboxylic acid] and a thiazide diuretic (chlorthalidone) would be more effective at lowering blood pressure and reducing renal injury in a rodent model of metabolic syndrome compared
Questions
Reviews
★★★★★ No rating value
Active Filters
Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.