In vitro, BQ-788 potently and competitively inhibited 125I-labeled ET-1 binding to ET-B receptors on human Girardi heart cells (IC50= 1.2 nM). However, BQ-788 only poorly inhibited ET-1 binding to ET-A receptors on human neuroblastoma cell line SK-N-MC cells (IC50= 1300 nM). Thus the ET-B receptor antagonist BQ788 may be considered as a powerful tool for investigating the role of ET in physiological and pathological processes.
Technical inquiry about: 01-4026108 BQ-788
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