conclusions we observed acceptable results regarding both efficacy and safety with 62.5 mg of bosentan, twice daily in this group of patients. further clinical trials investigating pah with lower dosages of bosentan may be warranted. results no adverse drug reaction was observed during the follow-up. clinical worsening occurred in six (14%) patients, at least one year after treatment, two of th...

Glomerular diseases are the leading cause of ESKD worldwide. IgA nephropathy (IgAN), focal segmental glomerulosclerosis (FSGS), Alport syndrome (AS), and diabetic kidney disease (DKD) important glomerular characterized by proteinuria, a predictor progression ESKD. Endothelin A (ETA) receptor activation drives inflammation, fibrosis. Therefore, atrasentan, potent selective ETA antagonist, has po...

Cochinmicins I, II, III are novel peptolides produced in submerged-fermentation cultures of Microbispora sp. ATCC 55140. These closely related compounds are separated by HPLC and are novel competitive endothelin antagonists. Cochinmicins II and III are stereoisomeric to each other. Cochinmicin I is the deschloro analog of cochinmicin III.

Tosun M, Erac Y, Selli C, Karakaya N. Sarcoplasmic-endoplasmic reticulum Ca -ATPase inhibition prevents endothelin A receptor antagonism in rat aorta. Am J Physiol Heart Circ Physiol 292: H1961–H1966, 2007. First published December 15, 2006; doi:10.1152/ajpheart.00298.2006.—This study tested whether sarcoplasmic-endoplasmic reticulum Ca -ATPase regulates the ability of endothelin receptor antag...

This study tested whether sarcoplasmic-endoplasmic reticulum Ca(2+)-ATPase regulates the ability of endothelin receptor antagonist to inhibit the endothelin-1 constriction. The endothelin A receptor antagonist BQ-123 (1 microM) completely relaxed constriction to 10 nM endothelin-1 in endothelium-denuded rat aorta. Challenge with cyclopiazonic acid (10 microM), a sarcoplasmic-endoplasmic reticul...

Endothelin is a potent vasoconstrictor peptide produced by endothelial cells, but its role in physiology and disease is uncertain. We investigated the influence of the endothelin-A-selective receptor antagonist PD 147953 and the nonselective endothelin receptor antagonist PD 145065 on the effects of endothelin-1 and endothelin-3 in the skin microcirculation of healthy volunteers, using laser Do...

Hypercholesterolemia is associated with increased circulating and tissue endothelin-1 immunoreactivity, decreased nitric oxide (NO) activity, and altered endothelial function. We tested the hypothesis that chronic endothelin receptor antagonism preserves endothelial function and increases NO in experimental porcine hypercholesterolemia. Pigs were randomized to 3 groups: Group 1, a 2% high-chole...

Background/aim Endothelin causes vasoconstriction via the endothelin-A receptor (ET-A) in intrahepatic circulation cirrhosis and its increase leads to portal hypertension. The aim of study was investigate acute effect a selective ET-A antagonist patients with hypertension cirrhosis. Methods Proof-of-concept two different substudies: (a) local administration BQ 123 (b) systemic oral Ambrisentan....