JNJ 31020028 Chemical Properties

Boiling point:

677.5±55.0 °C(Predicted)

Density 

1.228±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMSO : 21.5 mg/mL (38.01 mM; Need ultrasonic and warming)

form 

Powder

pka

12.14±0.70(Predicted)

JNJ 31020028 Usage And Synthesis

Description

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. 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 (IC₅₀ = 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 Y₂ 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.

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