BIBP3226 TFA is an effective and selective antagonist of neuropeptide Y Y1 (NPY Y1) and neuropeptide FF (NPFF) receptor (Kis: 1.1, 79, and 108 nM for rNPY Y1, hNPFF2, and rNPFF).
JNJ-5207787 is a penetrates the blood-brain barrier neuropeptide Y Y2 receptor (Y2) antagonist. It is >100-fold selective versus human Y1, Y4, and Y5 receptors. JNJ-5207787 suppresses the binding of peptide YY with pIC50s of 7.0 and 7.1 for the human Y2 r
Neuropeptide Y (NPY) (3-36) is a C-terminal fragment of NPY, a neuropeptide involved in controlling appetite, blood pressure, cardiac contractility, and intestinal secretion. NPY (3-36) is an endogenous peptide produced by cleavage of NPY by dipeptidyl peptidase 4 (DPP-4). It binds selectively to the NPY receptor Y2 (Ki = 0.41 nM in CHP 234 cells) over the Y1receptor, where it does not bind at concentrations up to 1 μM. NPY (3-36) (0.1 nM) increases migration of human umbilical vein endothelial cells (HUVECs) by 80% after 12 hours in an in vitro wound closure assay. NPY (3-36) corresponds to residues 3-36 of the human and rat protein sequence.
Potent, selective and competitive nonpeptide antagonist for the neuropeptide Y Y2 receptor (IC50 = 15 nM). Displays > 650-fold selectivity for NPY Y2 over Y1, Y4 and Y5 receptors. Active in vivo.
BIBP 3226 trifluoroacetate is a mixed non-peptide neuropeptide Y Y1(NPY Y1) and neuropeptide FF (NPFF) receptor antagonist (Kivalues are 1.1, 79, 108, > 1000, > 1000 and >1000 for rNPY Y1, hNPFF2, rNPFF, rNPY Y2, rNPY Y4and rNPY Y5respectively). Produces an anxiogenic-like effect in rats following i.c.v. administration.
BIIE-0246 is a potent, selective and competitive non-peptide antagonist for the neuropeptide Y Y2 receptor. BIIE-0246 displays > 650-fold selectivity over Y1, Y4 and Y5 receptors.
Potent, selective peptide agonist for the neuropeptide Y Y5 receptor (IC50 values for inhibition of NPY binding to human Y5, Y1, Y2 and Y4 receptors are 0.24, 530, > 500, and 51 nM respectively, Ki at Y5 = 0.1 - 0.15 nM). Stimulates food intake in vivo.