| Identification | Back Directory | [Name]
JNJ 31020028 | [CAS]
1094873-14-9 | [Synonyms]
CS-1745
JNJ 31020028
JNJ31020028, >98%
JNJ-31020028?, >98%
JNJ-31020028;JNJ 31020028
1-Piperazineacetamide, N,N-diethyl-4-[2-fluoro-4-[[2-(3-pyridinyl)benzoyl]amino]phenyl]-α-phenyl-
N,N-Diethyl-4-[2-fluoro-4-[[2-(3-pyridinyl)benzoyl]amino]phenyl]-alpha-phenyl-1-piperazineacetamide
N-(4-(4-(2-(diethylamino)-2-oxo-1-phenylethyl)piperazin-1-yl)-3-fluorophenyl)-2-(pyridin-3-yl)benzamide
4-[1-(BENZENESULFONYL)-4-(4,4,5,5-TETRAMETHYL-1,3,2-DIOXABOROLAN-2-YL)PYRROLO[2,3-B]PYRIDIN-2-YL]BENZALDEHYDE | [Molecular Formula]
C34H36FN5O2 | [MDL Number]
MFCD18782744 | [MOL File]
1094873-14-9.mol | [Molecular Weight]
565.68 |
| Chemical Properties | Back Directory | [Boiling point ]
677.5±55.0 °C(Predicted) | [density ]
1.228±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 21.5 mg/mL (38.01 mM; Need ultrasonic and warming) | [form ]
Powder | [pka]
12.14±0.70(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [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. 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. | [Uses]
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[1]. | [in vivo]
JNJ-31020028 (0-20 mg/kg; s.c. once) affects the level of plasma corticosterone and refeeding result in stressed animals[1]. | Animal Model: | Stressed and nonstressed male Sprague-Dawley rats[1] | | Dosage: | 0, 3, 10 and 20 mg/kg | | Administration: | Subcutaneous injection; 0-20 mg/kg once | | Result: | Significantly decreased plasma corticosterone levels in stressed animals, but not significantly affected plasma corticosterone levels in nonstressed animals. Attenuated effects of stress on refeeding. |
| [storage]
Store at -20°C | [References]
[1] Shoblock JR, 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 DOI:10.1007/s00213-009-1726-x |
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