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BMS 182874 hydrochloride
Other Information:
Sold
with the permission of Bristol-Myers Squibb Company, subject to U.
S.
Patent No.
5,378,715 and other US and foreign patents
Chemical Name:5-(Dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-napht
halenesulfonamide hydrochloride
Biological Activity:
Potent,
selective and competitive non-peptide endothelin ETA receptor
antagonist (Ki = 48 nM). Displays > 1000-fold selectivity over ETB
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.
Steinet al (1994)The
discovery of sulfonamide endothelin antagonists and the development of the
orally active ETA antagonist 5-(Dimethylamino)-N-(3,4-dimethyl-5-isoazolyl)-1-naphthalenesulfonamide.
37 329. Webbet al (1995) BMS-182874 is a
selective, nonpeptide endothelin ETA receptor antagonist.
J.Pharmacol.Exp.Ther. 272 1124. Khanet al (2006)
Pharmacological characterization of endothelin receptors-mediated contraction
in the mouse isolated proximal and distal colon. Br.J.Pharmacol. 147
607.
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