neuropeptide y1 receptor

BMS-193885 is a selective, brain-penetrant, and competitive antagonist of the neuropeptide Y1 receptor with a Ki of 3.3 nM, and an IC50 of 5.9 nM for hY1.

Y1 receptor antagonist 1 (H 409-22 isomer) is the active isomer of H-409 22, a neuropeptide Y (NPY) Y1 receptor antagonist that dose-dependently antagonizes the vascular response to exogenous and endogenous NPY in pigs. lagodeoxycholic acid (H 409-22 isomer) is the active isomer of H-409 22, an antagonist of neuropeptide Y (NPY) Y1 receptor.

BIBO3304 TFA is an effective, orally active, and selective neuropeptide Y (NPY) Y1 receptor antagonist (IC50:0.38 and 0.72 nM for the human and the rat Y1 receptor).

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

JNJ-31020028 is a selective brain penetrant antagonist of neuropeptide Y2 receptor with high affinity(pIC50=8.07, human; pIC50=8.22, rat); it exhibits >100-fold selectivity for Y2 versus human Y1 Y4 Y5 receptors.

H 409-22 isomer formic, a formate salt of Y1 receptor antagonist 1, is an antagonist of the neuropeptide Y1 receptor (neuropeptide Y1 receptor). This compound effectively blocks the actions of the receptor, playing a crucial role in modulating physiological responses.

BMS 193885 is a selective and competitive neuropeptide Y(1) receptor antagonist with affinity of 3.3 nM.

neuropeptide Y1 receptor antagonist

BIBP3226 is a potent and selective antagonist for the Neuropeptide Y receptor (Y1) and the neuropeptide FF receptor (NPFF).

CP-671906 is a neuropeptide Y1 receptor antagonist which increases blood pressure and food intake in rat models.

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 Y1 receptor, 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.

CGP71683 hydrochloride (CGP71683A) is a competitive neuropeptide Y5 receptor antagonist (Ki: 1.3 nM) and shows no obvious activity at Y1 receptor (Ki >4000 nM) and Y2 receptor (Ki: 200 nM) in cell membranes.

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.

Compound 39, also known as Y1R probe-1, is a high-affinity fluorescent probe targeting the Neuropeptide Y Y1 Receptor, with potential applications in cancer research [1].

[D-Arg25]-Neuropeptide Y (human) ([D-Arg25] NPY), a Y1 receptor selective agonist, is involved in Alzheimer's disease (AD) and protects rat cortical neurons from β-Amyloid toxicity [1].

[D-Trp34]-Neuropeptide Y TFA is a potent and selective agonist for the neuropeptide Y (NPY) Y5 receptor, demonstrating significantly lower potency at the NPY Y1, Y2, Y4, and Y6 receptors. It significantly increases food intake in rats [1] [2].

[Leu31,Pro34]-Neuropeptide Y(human,rat) TFA acts as a specific agonist for the neuropeptide Y Y1 receptor and also activates Y4 and Y5 receptors, elevating blood pressure in anesthetized rats and enhancing food intake [1] [2].

Neuropeptide Y (3-36) (porcine) acts as an agonist for the Y2 subtype of the neuropeptide Y (NPY) receptor, effectively stimulating feeding behavior in rats. This compound exhibits high selectivity for the Y2 receptor compared to the non-selective Y1 Y2 receptor ligand, Neuropeptide Y 1-36 [1][2][3].

BIBO3304 (diTFA), a selective neuropeptide Y (NPY) Y1 receptor antagonist, demonstrates oral efficacy. It exhibits high affinity for Y1 receptors in both humans and rats, with IC50 values of 0.38 nM and 0.72 nM, respectively. Additionally, BIBO3304 (diTFA) enhances bone-tendon healing via the Wnt/β-catenin signaling pathway [1] [2] [3].

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.

Potent neuropeptide Y (NPY) Y5 receptor agonist (pEC50 values are 7.82, 6.28, 6.44 and > 6 at rat Y5, Y4, Y1 and Y2 receptors respectively) that displays > 26-fold, > 1000-fold and > 1000-fold selectivity over Y1, Y2 and Y4 receptors respectively. Induces