An antagonist of NPY receptor Y2
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JNJ-31020028

Item No. 18407

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N,N-diethyl-4-[2-fluoro-4-[[2-(3-pyridinyl)benzoyl]amino]phenyl]-α-phenyl-1-piperazineacetamide
CAS Number
1094873-14-9
Molecular Formula
C34H36FN5O2
Formula Weight
565.7
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: >10 mg/ml
λmax
267 nm
SMILES
O=C(NC1=CC=C(N2CCN(C(C(N(CC)CC)=O)C3=CC=CC=C3)CC2)C(F)=C1)C4=CC=CC=C4C5=CN=CC=C5
InChi Code
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)
InChi Key
OVUNRYUVDVWTTE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    1 mg

    $75

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    5 mg

    $168

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    10 mg

    $295

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    25 mg

    $645

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    Product Description

    JNJ-31020028 is a brain-permeable selective antagonist of the neuropeptide Y (NPY) receptor Y2 (IC50s = 8.51, 6.03, and 6.17 nM for human, rat, and mouse receptors, respectively) with over 100-fold selectivity for Y2 over Y1, Y4, and Y5 receptors.1,2 JNJ-31020028 inhibits calcium release induced by peptide YY in a functional assay in KAN-TS cells (pKB = 8.04) and blocks NPY(13-36)-induced decreases in twitch contraction amplitude in isolated rat vas deferens (IC50 = 7.94 nM).1 Administration of JNJ-31020028 to rats during abstinence (20 mg/kg per day, i.p.) reverses nicotine-induced social anxiety-like behavior and increases hippocampal Y2 receptor mRNA levels.3 It reverses withdrawal-induced anxiety-like behavior in rats in the elevated plus maze following a single bolus dose of alcohol when administered at a dose of 15 mg/kg.4 In an olfactory bulbectomized rat model of depression, chronic JNJ-31020028 treatment (10 nmol per day, i.c.v.) decreases immobility time in the forced swim test but has no effect in control animals.5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Shoblock, J.R., Welty, N., Nepomuceno, D., et al. 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 Y2 receptor. Psychopharmacology (Berl) 208(2), 265-277 (2010).

    2. Swanson, D.M., Wong, V.D., Jablonowski, J.A., et al. The discovery and synthesis of JNJ 31020028, a small molecule antagonist of the Neuropeptide Y Y₂ receptor. Bioorg. Med. Chem. Lett. 21(18), 5552-5556 (2011).

    3. Aydin, C., Oztan, O., and Isgor, C. 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. Behav. Brain Res. 222(2), 332-341 (2011).

    4. Cippitelli, A., Rezvani, A.H., Robinson, J.E., et al. The novel, selective, brain-penetrant neuropeptide Y Y2 receptor antagonist, JNJ-31020028, tested in animal models of alcohol consumption, relapse, and anxiety. Alcohol 45(6), 567-576 (2011).

    5. Morales-Medina, J.C., Dumont, Y., Bonaventure, P., et al. Chronic administration of the Y2 receptor antagonist, JNJ-31020028, induced anti-depressant like-behaviors in olfactory bulbectomized rat. Neuropeptides 46(6), 329-334 (2012).