Uses
BIIE 0246, is a selective non-peptide antagonist which binds to the neuropeptide NPY2-R in a competitive manner. Studies have also shown that BIIE 0246 is highly lipophilic and as a result BIIE 0246 builds up at membranes near the receptors.
Biological Activity
Potent, selective and competitive non-peptide antagonist for the neuropeptide Y Y 2 receptor (IC 50 = 15 nM). Displays > 650-fold selectivity over Y 1 , Y 4 and Y 5 receptors. Active in vivo .
References
[1]. 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.
[2]. 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.
[3]. 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.
[4]. 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.
[5]. 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.
