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...

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...

Endothelins (ETs), 21-amino-acid peptides involved in the pathogenesis of various diseases, bind to ET(A) and ET(B) receptors to initiate their effects. Based on the same core structure, we have developed four small-molecule ET receptor antagonists, ABT-627 (atrasentan), ABT-546, A-182086 and A-192621, which exhibit differences in selectivity for ET(A) and ET(B) receptors. In this report, we co...

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...

Collecting duct (CD)-derived endothelin-1 (ET-1) acting via endothelin B (ETB) receptors promotes Na(+) excretion. Compromise of ET-1 signaling or ETB receptors in the CD cause sodium retention and increase blood pressure. Activity of the epithelial Na(+) channel (ENaC) is limiting for Na(+) reabsorption in the CD. To test for ETB receptor regulation of ENaC, we combined patch-clamp electrophys...

Endothelins (ETs), 21-amino-acid peptides involved in the pathogenesis of various diseases, bind to ET(A) and ET(B) receptors to initiate their effects. Based on the same core structure, we have developed four small-molecule ET receptor antagonists, ABT-627, ABT-546, A-182086 and A-192621, which exhibit difference in selectivity for ET(A) and ET(B) receptors. In this report, we compare the pote...

Background: Recent research has provided evidences indicating the importance of endothelin axis in carcinogenesis. According to our knowledge, there are little information about endothelin A receptor (ETA) expression in oral squamous cell carcinoma (OSCC). So, the aim of the present study was to evaluate the immunohistochemical expression of ETA in OSCC and normal oral mucosa (...

The structures of stachybocins A, B and C, new endothelin receptor antagonist, were determined by NMR spectral analysis using pulse-field-gradient technique. Stachybocin A consists of two spirobenzofuran units each fused to a substituted decalin, which were connected by a lysine residue. Stachybocins B and C are derivatives of stachybocin A with an additional hydroxy group at the same position ...

Background: Broilers lung mechanisms that regulate endothelin (ET) in the lung are complex and poorly understood. Objectives: Methods: In this experiment lung ET-1 mRNA levels and lung mRNA expression for the ET(A) receptors were determined in lung tissue weekly (term = 42 days, intervals = 7 days). Serum endothelin concentration was also measured at these ages. Results: The study showed that e...