Chemical Name:N-3-[1,1'-Biphenyl]-4-yl-N-(3,5-dimethylbenzoyl)-N-meth
yl-D-alanyl-L-tryptophan
Biological Activity:
Potent endothelin receptor antagonist; shows
some selectivity for ETB receptors (IC50 values are 1.3
and 94 nM for ETB and ETA receptors respectively).
Inhibits ETB receptor-mediated blood pressure increase and renal
vascular resistance in rats in vivo.
Balwierczaket al (1995) Characterization
of a potent and selective endothelin-B receptor antagonist, IRL 2500.
J.Cardiovasc.Pharmacol. 26 S393. Webbet al (1995)
Effects of the ETB-selective antagonist IRL 2500 in conscious
spontaneously hypertensive and Wistar-Kyoto rats. J.Cardiovasc.Pharmacol. 26
S389. Leung et al (2002) Use of A-192621 and IRL-2500 to unmask
the mesenteric and renal vasodilator role of endothelin ETB
receptors. J.Cardiovasc.Pharmacol. 39 533.