Endothelins (ETs), 21-amino-acid peptides involved in the pathogenesis of various diseases, bind to ETA and ETB 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 ETA and ETB receptors. In this report, we compare the potency and selectivity of these four antagonists in inhibiting 125I-labelled ET-1 binding to cloned human ETA and ETB receptors, and in blocking ET-1-induced functional responses (arachidonic acid release and phosphatidylinositol hydrolysis).
Pharmacology of endothelin receptor antagonists ABT-627, ABT-546, A-182086 and A-192621: in vitro studies
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J. Ruth WU-WONG, Douglas B. DIXON, William J. CHIOU, Brian K. SORENSEN, Gang LIU, H.-S. JAE, Andrew TASKER, Thomas W. Von GELDERN, Martin WINN, Terry J. OPGENORTH; Pharmacology of endothelin receptor antagonists ABT-627, ABT-546, A-182086 and A-192621: in vitro studies. Clin Sci (Lond) 1 September 2002; 103 (s2002): 107S–111S. doi: https://doi.org/10.1042/CS103S107S
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