1094873-14-9
1094873-14-9 structure
- Name: JNJ-31020028
- Chemical Name: N-[4-[4-[2-(diethylamino)-2-oxo-1-phenylethyl]piperazin-1-yl]-3-fluorophenyl]-2-pyridin-3-ylbenzamide
- CAS Number: 1094873-14-9
- Molecular Formula: C34H36FN5O2
- Molecular Weight: 565.680
- Catalog: Signaling Pathways GPCR/G Protein Neuropeptide Y Receptor
- Create Date: 2016-12-30 12:23:21
- Modify Date: 2024-01-03 12:48:02
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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].
| Name | N-[4-[4-[2-(diethylamino)-2-oxo-1-phenylethyl]piperazin-1-yl]-3-fluorophenyl]-2-pyridin-3-ylbenzamide |
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| Synonyms |
N-(4-{4-[2-(Diethylamino)-2-oxo-1-phenylethyl]-1-piperazinyl}-3-fluorophenyl)-2-(3-pyridinyl)benzamide
UNII:73F8XED6YP unii-73f8xed6yp 1-Piperazineacetamide, N,N-diethyl-4-[2-fluoro-4-[[2-(3-pyridinyl)benzoyl]amino]phenyl]-α-phenyl- JNJ 31020028 JNJ31020028 JNJ-31020028 |
| Description | 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]. |
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| Related Catalog | |
| References |
| Density | 1.2±0.1 g/cm3 |
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| Boiling Point | 677.5±55.0 °C at 760 mmHg |
| Molecular Formula | C34H36FN5O2 |
| Molecular Weight | 565.680 |
| Flash Point | 363.5±31.5 °C |
| Exact Mass | 565.285278 |
| PSA | 72.27000 |
| LogP | 5.23 |
| Appearance | white solid |
| Vapour Pressure | 0.0±2.1 mmHg at 25°C |
| Index of Refraction | 1.628 |
| Storage condition | -20℃ |
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1094873-14-9 |
| Literature: JANSSEN PHARMACEUTICA, N.V. Patent: WO2009/6185 A1, 2009 ; Location in patent: Page/Page column 35-36 ; WO 2009/006185 A1 |
| Precursor 1 | |
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| DownStream 0 | |