Potent
neuropeptide Y (NPY) Y1 receptor antagonist (pA2 = 10 and
10.5 at rY1 and hY1, receptors respectively). Also a
potent and selective NPY Y4 receptor agonist (pEC50
values are 6.0, 8.6 and 6.1 for rY2, hY4 and rY5
receptors respectively). Suppresses food intake in rats in vivo. Also has
affinity for neuropeptide FF (NPFF) receptors in vitro (Ki = 43-73
nM).
Parkeret al
(1998) GR231118 (1229U91) and other analogues of the C-terminus of neuropeptide
Y are potent neuropeptide Y Y1 receptor antagonists and neuropeptide
Y Y4 receptor agonists. Eur.J.Pharmacol. 349 97. Ishiharaet al (1998) A potent neuropeptide Y antagonist, 1229U91, suppressed
spontaneous food intake in Zucker fatty rats. Am.J.Physiol. 274 R1500.
Mollereauet al (2001) Agonist and antagonist activities on human
NPFF2 receptors of the NPY ligands GR231118 and BIBP3226.
Br.J.Pharmacol. 133 1.