| Description | (R)-JNJ-31020028 is a high affinity, selective brain penetrant antagonist of neuropeptide Y Y2 receptor(pIC50 values of 8.07, 8.22 and 8.21 for human, rat, and mouse Y2 receptor, respectively). |
| In vivo | Chronic icv administration of (R)-JNJ-31020028 at 5.6 μg/day using osmotic Alzet pump resulted in a significant decreases number of grooming events[1]. (R)-JNJ-31020028 treatment shows the Cmax, Tmax , AUCinf, Vd, and t1/2 were 4.35 μM, 0.5 hours, 7.91 h μM and 0.83 hours, respectively. (R)-JNJ-31020028 has antidepressant like effects in the olfactory bulbectomized rat (OBX) model. [1]. |
| Target activity | Y2 receptor (mouse):8.21(pIC50), Y2 receptor (human):8.07(pIC50), Y2 receptor (rat):8.22(pIC50) |
| molecular weight | 565.68 |
| Molecular formula | C34H36FN5O2 |
| CAS | 1094873-17-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| 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 Y(2) receptor. Psychopharmacology (Berl). 2010 Feb;208(2):265-77. 2. Morales-Medina JC, et al. Chronic administration of the Y2 receptor antagonist, JNJ-31020028, induced anti-depressant like-behaviors in olfactory bulbectomized rat. Neuropeptides. 2012 Dec;46(6):329-34. |