JNJ-31020028

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. 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). 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. 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. 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.Formal Name: N,N-diethyl-4-[2-fluoro-4-[[2-(3-pyridinyl)benzoyl]amino]phenyl]-alpha-phenyl-1-piperazineacetamide. CAS Number: 1094873-14-9. Molecular Formula: C34H36FN5O2. Formula Weight: 565.7. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: >10 mg/ml. lambdamax: 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.