Neuropeptide Y Receptor Antagonist

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.

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).

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

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.

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.

Galantide TFA is a reversible and non-specific galanin (GAL) receptor antagonist. Galantide TFA dose-dependently shows antagonism to galanin-induced K⁺ conductance with an IC₅₀ value of 4 nM. Galantide TFA can be used for the research of neurological disease and hormone metabolism research.

BIBP3226 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 displays anxiogenic-like effect.

Neuropeptide Y (18-36) (porcine) is a competitive neuropeptide Y (NPY) cardiac receptor antagonist. Neuropeptide Y (18-36) (porcine) inhibits the binding of I-NPY to cardiac ventricular membranes in a concentration-dependent manner with an IC₅₀ value of 158 nM and an K_i value of 140 nM. Neuropeptide Y (18-36) (porcine) can be used for the research of congestive heart failure.

SF-22 is a potent and brain-penetrant antagonist of neuropeptide Y receptor (Y2R), with the IC₅₀ value of 750 nM. SF-22 plays an important role in neurological disease.

S 25585 is a potent and selective neuropeptide Y (NPY) Y5 receptor antagonist. S 25585 reduces food intake but not through blockade of the NPY Y5 receptor.

BIIE-0246 hydrochloride (AR-H 053591 hydrochloride) 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 hydrochloride decreases the expression of p-AKT S473, P-p44/42 MAPK under the NPY-stimulated. BIIE-0246 hydrochloride reduces albuminuria in ADR nephropathy.

Peptide YY (PYY) (3-36), porcine is a gut hormone peptide that acts as a Y2 receptor agonist to reduce appetite.

Galantide, a non-specific galanin receptor antagonist, is a peptide consisting of fragments of galanin and substance P. Galantide recognizes two classes of galanin binding sites (K_D<0.1 nM and ~6 nM) in the rat hypothalamus. Galantide dose dependently (IC₅₀=1.0 nM) antagonizes the galanin-mediated inhibition of the glucose-induced insulin secretion from mouse pancreatic islets. Galantide appears to bind to a single population of SP receptors (K_D~40 nM).

NPY-5 receptor antagonist-1 (Example 57) is a NPY-5 receptor antagonist (K_i: < 1 μM). NPY-5 receptor antagonist-1 can be used for research of obesity, feeding disorders, as well as other neurological diseases.

BVD 10, a neuropeptide Y (NPY) analogue peptide, is a highly selective NPY Y1 receptor antagonist. BVD10 significantly prevents NPY-induced glutamate increase. BVD 10 can be used for seizure research.

CGP 71683 Free base serves as a powerful and highly selective non-peptide antagonist targeting the NPY Y(5) receptor, making it a valuable tool in obesity research.

human GALP (3-32) (Galanin-like peptide (3-32)) is a potent galanin receptor agonist with high affinity for both GalR1 (IC₅₀=33 nM) and GalR2 (IC₅₀=15 nM) in a competitive binding study. human GALP (3-32) exhibits the high potency in altering the extracellular acidification rate of SH-SY5Y cells transfected with GalR2 (EC₅₀=360 nM).