JNJ-31020028


CAS No. : 1094873-14-9

JNJ-31020028,1094873-14-9
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000400
Synonyms:N-[4-[4-[2-(diethylamino)-2-oxo-1-phenylethyl]piperazin-1-yl]-3-fluorophenyl]-2-pyridin-3-ylbenzamide
Molecular Formula:C₃₄H₃₆FN₅O₂
Molecular Weight:565.68
Target:Neuroscience Peptides
IC50:8.07/8.22(human/rat pIC50) [1]
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Appearance:White to off-white solid powder
Purity: > 98%
Cat No:I000400
Cas No:1094873-14-9
Product-Name:JNJ-31020028
InChI:InChI=1S/C34H36FN5O2/c1-3-38(4-2)34(42)32(25-11-6-5-7-12-25)40-21-19-39(20-22-40)31-17-16-27(23-30(31)35)37-33(41)29-15-9-8-14-28(29)26-13-10-18-36-24-26/h5-18,23-24,32H,3-4,19-22H2,1-2H3,(H,37,41)
InChIKey:OVUNRYUVDVWTTE-UHFFFAOYSA-N
SMILES:CCN(CC)C(=O)C(C1=CC=CC=C1)N2CCN(CC2)C3=C(C=C(C=C3)NC(=O)C4=CC=CC=C4C5=CN=CC=C5)F

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 antagonist
in 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].


1:PET brain imaging of neuropeptide Y2 receptors using N-11C-methyl-JNJ-31020028 in pigs. Winterdahl M, Audrain H, Landau AM, Smith DF, Bonaventure P, Shoblock JR, Carruthers N, Swanson D, Bender D.J Nucl Med. 2014 Apr;55(4):635-9. doi: 10.2967/jnumed.113.125351. Epub 2014 Mar 10. PMID: 24614224 Free Article
2:Chronic administration of the Y2 receptor antagonist, JNJ-31020028, induced anti-depressant like-behaviors in olfactory bulbectomized rat. Morales-Medina JC, Dumont Y, Bonaventure P, Quirion R.Neuropeptides. 2012 Dec;46(6):329-34. doi: 10.1016/j.npep.2012.09.009. Epub 2012 Oct 25. PMID: 23103057
3:The discovery and synthesis of JNJ 31020028, a small molecule antagonist of the Neuropeptide Y Y₂ receptor. Swanson DM, Wong VD, Jablonowski JA, Shah C, Rudolph DA, Dvorak CA, Seierstad M, Dvorak LK, Morton K, Nepomuceno D, Atack JR, Bonaventure P, Lovenberg TW, Carruthers NI.Bioorg Med Chem Lett. 2011 Sep 15;21(18):5552-6. doi: 10.1016/j.bmcl.2011.06.136. Epub 2011 Jul 18. PMID: 21802951
4:Effects of a selective Y2R antagonist, JNJ-31020028, on nicotine abstinence-related social anxiety-like behavior, neuropeptide Y and corticotropin releasing factor mRNA levels in the novelty-seeking phenotype. Aydin C, Oztan O, Isgor C.Behav Brain Res. 2011 Sep 23;222(2):332-41. doi: 10.1016/j.bbr.2011.03.067. Epub 2011 Apr 8. PMID: 21497168 Free PMC Article
5:The novel, selective, brain-penetrant neuropeptide Y Y2 receptor antagonist, JNJ-31020028, tested in animal models of alcohol consumption, relapse, and anxiety. Cippitelli A, Rezvani AH, Robinson JE, Eisenberg L, Levin ED, Bonaventure P, Motley ST, Lovenberg TW, Heilig M, Thorsell A.Alcohol. 2011 Sep;45(6):567-76. doi: 10.1016/j.alcohol.2010.09.003. Epub 2010 Dec 10. PMID: 21145691
6:In vitro and in vivo characterization of JNJ-31020028 (N-(4-{4-[2-(diethylamino)-2-oxo-1-phenylethyl]piperazin-1-yl}-3-fluorophenyl)-2-pyridin-3-ylbenzamide), a selective brain penetrant small molecule antagonist of the neuropeptide Y Y(2) receptor. Shoblock JR, Welty N, Nepomuceno D, Lord B, Aluisio L, Fraser I, Motley ST, Sutton SW, Morton K, Galici R, Atack JR, Dvorak L, Swanson DM, Carruthers NI, Dvorak C, Lovenberg TW, Bonaventure P.Psychopharmacology (Berl). 2010 Feb;208(2):265-77. doi: 10.1007/s00213-009-1726-x. Epub 2009 Dec 2. PMID: 19953226
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