Uses
BMS 182874 Hydrochloride, is a potent, selective, and competitive non-peptide endothelin ETAR antagonist (Ki = 48 nM). ET-A receptors are predominantly detected in peripheral tissues, especially in vascular smooth muscle tissues where they mediate vasoconstriction.
Definition
ChEBI: 5-(dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulfonamide is a member of naphthalenes and a sulfonic acid derivative.
Biological Activity
Potent, selective and competitive non-peptide endothelin ET A receptor antagonist (K i = 48 nM). Displays > 1000-fold selectivity over ET B receptors. Inhibits ET-1-induced pressor response following oral or intravenous administration in vivo . In vitro inhibits ET-1-induced longitudinal muscle contraction in the mouse colon.
