The endothelin (ET) family of proteins mediate a variety of responses, with ET-1 being a potent and long-lasting constrictor of human cardiovascular vessels.{28375} These proteins activate the G protein-coupled receptors ETA and ETB, with ETB being non-specific for ET protein form.{28375} BQ-788 is a potent, selective antagonist of ETB (IC50 = 1.2 nM for blocking ET-1 binding to human Girardi heart cells).{28374} It weakly inhibits the binding of ET-1 to ETA receptors on human neuroblastoma SK-N-MC cells (IC50 = 1300 nM).{28374} BQ-788 competitively antagonizes the vasoconstriction induced by an ETB-selective agonist on isolated rabbit pulmonary arteries, blocks ET-1 induced bronchoconstriction in guinea pigs, and abolishes an ET-1 mediated depressor response in rats.{28374}
产品描述
A potent, selective antagonist of ETB (IC50 = 1.2 nM for blocking ET-1 binding to human Girardi heart cells); competitively antagonizes the vasoconstriction induced by an ETB-selective agonist on isolated rabbit pulmonary arteries
