JNJ-31020028 – 1 mg

Brand:
Cayman
CAS:
1094873-14-9
Storage:
-20
UN-No:
Non-Hazardous - /

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.{38509,38510} 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).{38509} 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.{38511} 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.{38512} 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.{38515}  

 

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Description

An antagonist of NPY receptor Y2 (IC50s = 8.51, 6.03, and 6.17 nM for human, rat, and mouse receptors, respectively); 100-fold selective for Y2 over Y1, Y4, and Y5 receptors; inhibits calcium release induced by peptide YY in a functional assay in KAN-TS cells (pKB = 8.04); blocks NPY(13-36)-induced decreases in twitch contraction amplitude in isolated rat vas deferens (IC50 = 7.94 nM); reverses nicotine-induced social anxiety-like behavior in rats when administered during abstinence at a dose of 20 mg/kg per day, i.p., and increases hippocampal Y2 receptor mRNA levels; reverses withdrawal-induced anxiety-like behavior in rats from a single bolus dose of alcohol in the elevated plus maze when used at a dose of 15 mg/kg, s.c.; chronic administration in an olfactory bulbectomized rat model of depression decreases immobility time in the forced swim test but has no effect in control animals when used at a dose of 10 nmol per day, i.c.v.


Formal name: N,N-diethyl-4-[2-fluoro-4-[[2-(3-pyridinyl)benzoyl]amino]phenyl]-α-phenyl-1-piperazineacetamide

Synonyms: 

Molecular weight: 565.7

CAS: 1094873-14-9

Purity: ≥95%

Formulation: A crystalline solid


Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Neuroscience|Behavioral Neuroscience|Addiction Research||Research Area|Neuroscience|Behavioral Neuroscience|Anxiety||Research Area|Neuroscience|Behavioral Neuroscience|Depression