Chemical Name:N-[(1S)-4-[(Aminoiminomethyl)amino]-1-[[[2-(3,5-dioxo-1
,2-diphenyl-1,2,4-triazolidin-4-yl)ethyl]amino]carbonyl
]butyl]-1-[2-[4-(6,11-dihydro-6-oxo-5H-dibenz[b,e]azepi
n-11-yl)-1-piperazinyl]-2-oxoethyl]-cyclopentaneacetami
de formate
Biological Activity:
Potent,
selective and competitive non-peptide antagonist for the neuropeptide Y Y2
receptor (IC50 = 15 nM). Displays > 650-fold selectivity over Y1,
Y4 and Y5 receptors. Active in vivo.
Doodset al (1999) BIIE0246: a
selective and high affinity neuropeptide Y Y2 receptor antagonist.
Eur.J.Pharmacol. 384 R3. Dumont et al (2000)
BIIE0246, a potent and highly selective non-peptide neuropeptide Y Y2
receptor antagonist. Br.J.Pharmacol. 129 1075. Malmstrom
(2001) Vascular pharmacology of BIIE0246, the first selective non-peptide
neuropeptide Y Y2 receptor antagonist, in vivo.
Br.J.Pharmacol. 133 1073.
![BIIE 0246 C49H57N11O6.CH2O2 N-[(1S)-4-[(Aminoiminomethyl)amino]-1-[[[2-(3,5-dioxo-1,2-diphenyl-1,2,4-triazolidin-4-yl)ethyl]amino]carbonyl]butyl]-1-[2-[4-(6,11-dihydro-6-oxo-5H-dibenz[b,e]azepin-11-yl)-1-piperazinyl]-2-oxoethyl]-cyclopentaneacetamide formate](image.php?ItemId=65309)
