PeptideDB

(R)-JNJ-31020028

CAS: 1094873-17-2 F: C34H36FN5O2 W: 565.68

(R)-JNJ-31020028 is a high affinity, selective brain penetrant neuropeptide Y Y2 receptor antagonist, with pIC50 values
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Bioactivity (R)-JNJ-31020028 is a high affinity, selective brain penetrant neuropeptide Y Y2 receptor antagonist, with pIC50 values of 8.07, 8.22 and 8.21 for human, rat, and mouse Y2 receptor, respectively. (R)-JNJ-31020028 shows >100-fold selective versus human Y1, Y4, and Y5 receptors. (R)-JNJ-31020028 has antidepressant like effects[1][2].
In Vivo (R)-JNJ-31020028 (5.6 μg; chronic icv infusion; daily for 10 days) has antidepressant like effects in the olfactory bulbectomized rat (OBX) model[1].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[1]. Animal Model:
Name (R)-JNJ-31020028
CAS 1094873-17-2
Formula C34H36FN5O2
Molar Mass 565.68
Transport Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Reference [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 [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.