Neuropeptide Y Receptor Antagonist

BIBO3304, a chemical probe, is a potent, orally active, and selective neuropeptide Y (NPY) Y1 receptor antagonist, with subnanomolar affinity for both the human and the rat Y1 receptor (IC₅₀=0.38 and 0.72 nM, respectively).

Allo-aca, a leptin peptidomimetic, is a potent, specific leptin receptor antagonist peptide. Allo-aca blocks leptin signaling and action in numerous in vitro and in vivo models.

BIIE-0246 (AR-H 053591) is a potent and selective NPY2R (neuropeptide Y receptor 2) antagonist with an IC₅₀ value of 15 nM for rat [¹²⁵I]PYY_3-36. BIIE-0246 decreases the expression of p-AKT S473, P-p44/42 MAPK under the NPY-stimulated. BIIE-0246 reduces albuminuria in ADR nephropathy.

BIBP3226 TFA is a potent and selective neuropeptide Y Y1 (NPY Y1) and neuropeptide FF (NPFF) receptor antagonist, with K_is of 1.1, 79, and 108 nM for rNPY Y1, hNPFF2, and rNPFF, respectively. BIBP3226 TFA displays anxiogenic-like effect.

SR 142948 is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC₅₀s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 shows blood-brain permeability and can be used in study of psychiatric disorders.

SR 142948A is a blood-brain barrier-permeable, orally active, selective, non-peptide Neurotensin Receptor antagonist. SR 142948A exhibits an IC₅₀ of 4.0 nM at the NTS1 site. SR 142948A competitively antagonizes neurotensin-dependent neurotransmitter release and modulates neurotensin-related dopaminergic and serotonergic signaling, making it useful for research on neurobehavioral mechanisms associated with schizophrenia.

JNJ-31020028 is a selective and brain penetrant antagonist of neuropeptide Y Y2 receptor with pIC₅₀ values of 8.07 and 8.22 for human and rat Y2 receptor, respectively. JNJ-31020028 can be used for the research of nervous disease.

M871 (Galanin-(2-13)-Glu-His-(Pro)3-(Ala-Leu)2-Ala-amide) is an orally active and selective galanin receptor type 2 (GalR2) antagonist. M871 exhibits K_i values of 13.1 nM, 420 nM and >10 μM for GalR2, GalR1 and GalR3 respectively. M871 relieves the mice allergic rhinitis by reducing IgE production, as well as the number of B cells in tissues. M871 can inhibit the nerve invasion of salivary adenoid cystic carcinoma (SACC) and alleviate myocardial ischemia-reperfusion injury. M871 can be used for research on GalR2-related diseases (such as epilepsy, pain).

MK-0557 is a highly selective, orally available neuropeptide Y5 receptor antagonist with a K_i of 1.6 nM.

HT-2157 (SNAP 37889) is a selective, high-affinity, competitive antagonists of galanin-3 receptor (Gal₃).

RF9 is a potent and selective Neuropeptide FF receptor antagonist, with K_i values of 58 and 75 nM for hNPFF1R and hNPFF2R, respectively.

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

BMS-193885 is a selective neuropeptide Y1 receptor antagonist (K_i=3.3 nM) that competitively blocks the receptor to inhibit NPY-mediated appetite regulation signaling pathways, reduce food intake and inhibit weight gain. BMS-193885 has good blood-brain barrier penetration and is mainly used in the study of obesity and related metabolic diseases.

NTNCB (Compound 11) hydrochloride is a potent and selective neuropeptide Y Y5 (NPY Y5) receptor antagonist with a K_i of 8 nM against human Y5.

Galanin Receptor Ligand M35 is a high-affinity ligand and antagonist of galanin receptor (K_d=0.1 nM). Galanin Receptor Ligand M35 exerts a K_i values of 0.11 and 2.0 nM for human galanin receptor type 1 and 2, respectively.

Velneperit (S-2367) is an orally active neuropeptide Y (NPY) Y5 receptor antagonist that can penetrate the blood-brain barrier. Velneperit inhibits the appetite-stimulating and metabolism-inhibiting effects mediated by NPY. Velneperit selectively improves diet-induced obesity in mice. Velneperit enhances the expression of fear acutely by removing the inhibition of CeA Drd2 neurons. Velneperit can be used for the study of obesity.

CYM 9484 is a selective and highly potent neuropeptide Y (NPY) Y2 receptor antagonist with an IC₅₀ value of 19 nM.

L 152804 is an orally active and selective neuropeptide Y Y5 receptor (NPY5-R) antagonist, with a K_i of 26 nM for hY5. L 152804 causes weight loss in diet-induced obese mice by modulating food intake and energy expenditure.

SF 11 is a potent and brain penetrant neuropeptide Y Y2 receptor antagonist (IC₅₀=199 nM). Antidepressant-like activity.

NPY5RA-972 is an orally active, central nervous system (CNS) penetrating, potent and selective NPY Y5 receptor antagonist that prevents feeding driven by activation of this receptor.