(R)-JNJ-31020028 is a high affinity, selective brain penetrant neuropeptide Y Y2 receptor antagonist, with pIC50 values of 8.07, 8.22 and 8.21 for human, rat, and mouse Y2 receptor, respectively. (R)-JNJ-31020028 shows >100-fold selective versus human Y1, Y4, and Y5 receptors. (R)-JNJ-31020028 has antidepressant like effects[1][2].
Velneperit (S-2367) is a novel neuropeptide Y (NPY) Y5 receptor antagonist.Target: neuropeptide Y receptorVelneperit (S-2367) is a once-daily, oral, centrally acting, small molecule neuropeptide Y (NPY) Y5 receptor antagonist.
BIBO3304 TFA 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)[1].
Neuropeptide Y5 receptor ligand-1 (compound 54), a carbazole derivative, is a potent neuropeptide Y5 (NPY-5) receptor antagonist[1].
[Leu31,Pro34]- Neuropeptide Y (porcine), a Neuropeptide Y (NPY) analog, is a selective NPY Y1 receptor agonist. [Leu31,Pro34]- Neuropeptide Y (porcine) exhibits anxiolytic effects[1][2].
[Leu31,Pro34]-Neuropeptide Y(human,rat) is a specific neuropeptide Y Y1 receptor agonist. [Leu31,Pro34]-Neuropeptide Y(human,rat) slao inhibits Y4, Y5. [Leu31,Pro34]-Neuropeptide Y(human,rat) can increase blood pressure in anesthetized rats and increases food intake[1][2].
GR231118, an analogue of the C-terminus of neuropeptide Y, is a potent , competitive and relative seletive antagonist at human neuropeptide Y Y receptor with a pKi of 10.4. GR231118 a potent agonist at the human neuropeptide Y Y4 receptor (pEC50=8.6; pKi=9.6) and a weak agonist at the human and rat neuropeptide YY2 and Y5 receptors. GR231118 also has high affinity for the mouse neuropeptide Y Y6 receptor (pKi= 8.8)[1].
Galanin (1-13)-Neuropeptide Y (25-36) amide is a high-affinity ligand for galanin receptors, and galanin itself[1].
Peptide YY (PYY) is a gut hormone that regulates appetite and inhibits pancreatic secretion. Peptide YY (PYY) can mediate its effects through the Neuropeptide Y receptors.
Arginine vasopressin (AVP, also known as antidiuretic hormone (ADH)) is a 9 amino acid neuropeptide secreted by the posterior pituitary. AVP can regulate the biological effects of fluid balance, osmolality and cardiovascular through three separate G-protein coupled receptors (GPCRs), namely Avpr1a (V1a), Avpr1b (V1b) and Avpr2 (V2). AVP also have potentially important effects on centrally regulated metabolic processes[1].
Pancreatic Polypeptide, rat is an agonist of NPY receptor, with high affinity at NPYR4.
Galantide is a reversible and non-specific galanin receptor antagonist.
JNJ-31020028 is a selective brain penetrant antagonist of neuropeptide Y2 receptor with high affinity(pIC50=8.07, human; pIC50=8.22 rat); >100-fold selective versus human Y1/Y4/Y5 receptors.IC50 value: 8.07/8.22(human/rat pIC50) [1]Target: Y2 receptor antagonistin vitro: JNJ-31020028 was demonstrated to be an antagonist (pK(B) = 8.04 +/- 0.13) in functional assays [1].in vivo: JNJ-31020028 occupied Y(2) receptor binding sites (approximately 90% at 10 mg/kg) after subcutaneous administration in rats [1]. Neither systemic (0, 15, 30, and 40 mg/kg, subcutaneously [s.c.]) nor intracerebroventricular (0.0, 0.3, and 1.0 nmol/rat) administration of JNJ-31020028 affected alcohol-reinforced lever pressing or relapse to alcohol seeking behavior following stress exposure. JNJ-31020028 (15 mg/kg, s.c.) did reverse the anxiogenic effects of withdrawal from a single bolus dose of alcohol on the elevated plus-maze, confirming the anxiolytic-like properties of NPY Y2 antagonism [2]. Chronic administration of JNJ-31020028 induced a decrease in immobility time in the forced swim test in OBX while had no effect in control animals [3].
Neuropeptide Y (3-36) (human, rat), a neuropeptide Y (NPY) metabolite formed from dipeptidyl peptidase-4 (DPP4), is a selective Y2 receptor agonist. Neuropeptide Y (3-36) (human, rat) is a NPY metabolite formed from dipeptidyl peptidase-4 (DPP4). Neuropeptide Y (3-36) (human, rat) decreases release of norepinephrine via the Y2 receptor[1][2].
Neuropeptide Y (13-36), amide, human is a neuropeptide Y receptor agonist.
BMS-193885 (L-Lactic acid) is a potent, selective, and brain-penetrant neuropeptide Y1 receptor antagonist. BMS-193885 has a Ki value of 3.3 nM for the neuropeptide Y1 receptor, competitively acts on the neuropeptide Y binding site, and can reduce food intake and body weight through central Y1 inhibition[1].
(Pro34)-Peptide YY (human) is a highly Y1-selective full agonist of Peptide YY (HY-P1514)/neuropeptide Y receptors[1].
Galanin Receptor Ligand M35 is a high-affinity galanin receptor ligand acting as a galanin receptor antagonist in the rat spinal cord, rat hippocampus and isolated mouse pancreatic islets. Galanin Receptor Ligand M35 exerts a Ki values of 0.11 and 2.0 nM for human GalR1 and GalR2, respectively[1][2].
Lu AA33810 is a potent and selective antagonist of neuropeptide Y5 receptor with a Ki of 1.5 nM for the human receptor. Lu AA33810 exhibts antianxiolytic-like and antidepressant-like effects[1].
CART (55-76), rat is a neuropeptide (55-76 residues of the CART peptide) and constitutes the N-terminal fragments of CART (55-102). CART (55-76), rat is a rat satiety factor with potent appetite-suppressing activity and is closely associated with leptin and neuropeptide Y. CART (55-76), rat can induce anxiety and stress-related behavior[1].
[cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide is a potent and selective neuropeptide Y Y5 receptor agonist with an IC50 of 0.24 nM for binding to the hY5 receptor. [cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide induces a high amount of food intake[1].
JNJ-5207787 is a nonpeptidic, selective and penetrate the blood-brain barrier neuropeptide Y Y2 receptor (Y2) antagonist. JNJ-5207787 inhibits the binding of peptide YY (PYY) with pIC50s of 7.0 and 7.1 for human Y2 receptor and rat Y2 receptor, respectively. JNJ-5207787 is >100-fold selective versus human Y1, Y4, and Y5 receptors[1].
M871 (Galanin-(2-13)-Glu-His-(Pro)3-(Ala-Leu)2-Ala-amide) is a selective galanin receptor type 2 (GalR2) antagonist. M871 exhibits Ki values of 13.1 nM and 420 nM for GalR2 and GalR1, respectively. M871 can be used for research on GalR2-related diseases (such as epilepsy, pain)[1].
L 152804 is an orally active and selective neuropeptide Y Y5 receptor (NPY5-R) antagonist, with a Ki of 26 nM for hY5. L 152804 causes weight loss in diet-induced obese mice by modulating food intake and energy expenditure[1][2].
Peptide YY (pig) is a 36 amino acid gastrointestinal peptide, can be isolated from porcine duodenum. Peptide YY (pig) decreases appetite and food-intake by activation of the Y2 receptor. Peptide YY (pig) is present mainly in pancreatic endocrine cells with effect on both intestinal motility and the cardiovascular system[1][2][3].
(Leu31,Pro34)-Peptide YY (human) is a Peptide YY (HY-P1514) derivative and is a potent and selective Y1 agonist with a KD of 1.0 nM[1].
RTI-118 is a novel small-molecule neuropeptide S receptor (NPSR) antagonist. RTI-118 can relieve drug addiction including selectively decrease cocaine self-administration[1].
BIBP3226 TFA is a potent and selective neuropeptide Y Y1 (NPY Y1) and neuropeptide FF (NPFF) receptor antagonist, with Kis of 1.1, 79, and 108 nM for rNPY Y1, hNPFF2, and rNPFF, respectively. BIBP3226 TFA displays anxiogenic-like effect[1][2].
RFRP-3 (Neuropeptide VF(124-131))(human), a human GnIH peptide homolog, is a potent inhibitor of gonadotropin secretion by inhibiting Ca2+ mobilization. RFRP-3(human) is a NPFF1 receptor agonist, it inhibits forskolin-induced production of cAMP with an IC50 of 0.7 nM[1].
NTNCB (Compound 11) hydrochloride is a potent and selective neuropeptide Y Y5 (NPY Y5) receptor antagonist with a Ki of 8 nM against human Y5[1].