BIIE 0246 is a potent and selective antagonist of neuropeptide Y Y2 receptor with IC50 value of 3.3 nM .
Neuropeptide Y Y2 receptor (Y2R) is a G-protein-coupled receptor for neuropeptide Y (NPY), which is widely distributed in the peripheral and central nervous system. Y2R mediates the presynaptic inhibitory effect .
BIIE 0246 is a potent and selective Y2R antagonist. In rat hippocampal slices, BIIE0246 (100 nM) suppressed the inhibition of primary afterdischarge activity induced by NPY and [ahx5-24]NPY. Also, BIIE0246 suppressed the inhibitory effects of NPY and [ahx5-24]NPY, which inhibited the population excitatory postsynaptic potential (pEPSP) evoked by stratum radiatum stimulation in area CA1 . In HEK293 cells transfected with the rat Y2 receptor, BIIE0246 exhibited high affinity for specific PYY3-36 binding sites with Ki values of 8-15 nM. In the rat colon, BIIE0246 (1 μM) completely blocked PYY3-36-induced contraction response .
In rats, BIIE0246 (1 nM) attenuated the reduction in feeding induced by PYY(3-36) (7.5 nmol/kg). In satiated rats, BIIE0246 significantly increased feeding. These results suggested that Y2R played a critical role in post-prandial satiety . In the elevated plus-maze, BIIE0246 exhibited anxiolytic-like effect .
. Doods H, Gaida W, Wieland HA, et al. BIIE0246: a selective and high affinity neuropeptide Y Y(2) receptor antagonist. Eur J Pharmacol, 1999, 384(2-3): R3-5.
. El Bahh B, Cao JQ, Beck-Sickinger AG, et al. Blockade of neuropeptide Y(2) receptors and suppression of NPY's anti-epileptic actions in the rat hippocampal slice by BIIE0246. Br J Pharmacol, 2002, 136(4): 502-509.
. Dumont Y, Cadieux A, Doods H, et al. BIIE0246, a potent and highly selective non-peptide neuropeptide Y Y(2) receptor antagonist. Br J Pharmacol, 2000, 129(6): 1075-1088.
. Abbott CR, Small CJ, Kennedy AR, et al. Blockade of the neuropeptide Y Y2 receptor with the specific antagonist BIIE0246 attenuates the effect of endogenous and exogenous peptide YY(3-36) on food intake. Brain Res, 2005, 1043(1-2): 139-144.
. Bacchi F, Mathé AA, Jiménez P, et al. Anxiolytic-like effect of the selective neuropeptide Y Y2 receptor antagonist BIIE0246 in the elevated plus-maze. Peptides, 2006, 27(12): 3202-3207.
|Physical Appearance||White solid|
|Storage||Store at 4°C|
|Solubility||<67.2mg/ml in DMSO; <23.55mg/ml in ethanol|
|Canonical SMILES||O=C(CC1(CC(N[[email protected]](C(NCCN2C(N(C3=CC=CC=C3)N(C4=CC=CC=C4)C2=O)=O)=O)CCC/N=C(N)\N)=O)CCCC1)N5CCN([[email protected]@H](C6=CC=CC=C67)C8=CC=CC=C8NC7=O)CC5|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|