Description
JNJ-31020028 is a brain-permeable selective antagonist of the neuropeptide Y (NPY) receptor Y
2 (IC
50s = 8.51, 6.03, and 6.17 nM for human, rat, and mouse receptors, respectively) with over 100-fold selectivity for Y
2 over Y
1, Y
4, and Y
5 receptors. JNJ-31020028 inhibits calcium release induced by peptide YY in a functional assay in KAN-TS cells (pK
B = 8.04) and blocks NPY(13-36)-induced decreases in twitch contraction amplitude in isolated rat vas deferens (IC
50 = 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 Y
2 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].
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
