JNJ31020028|JNJ-31020028 neuropeptide Y2 receptor antagonist

JNJ31020028|JNJ-31020028 neuropeptide Y2 receptor antagonist|DC Chemicals
JNJ-31020028 is a selective brain penetrant antagonist of neuropeptide Y2 receptor with high affinity(pIC50=8.07, human; pIC50=8.22 rat); >100-fold selective versus human Y1/Y4/Y5 receptors.

Product name: JNJ31020028 |Cat No. DC8140|Other names: JNJ31020028,JNJ-31020028,JNJ 31020028|Cas: 1094873-14-9|Molecule Weight: 565.68|Molecule Formular: C34H36FN5O2| Purity: >98%

JNJ-31020028 bound with high affinity (pIC(50) = 8.07 +/- 0.05, human, and pIC(50) = 8.22 +/- 0.06, rat) and was >100-fold selective versus human Y(1), Y(4), and Y(5) receptors. JNJ-31020028 was demonstrated to be an antagonist (pK(B) = 8.04 +/- 0.13) in functional assays. JNJ-31020028 occupied Y(2) receptor binding sites (approximately 90% at 10 mg/kg) after subcutaneous administration in rats. JNJ-31020028 increased norepinephrine release in the hypothalamus, consistent with the colocalization of norepinephrine and neuropeptide Y. In a variety of anxiety models, JNJ-31020028 was found to be ineffective, although it did block stress-induced elevations in plasma corticosterone, without altering basal levels, and normalized food intake in stressed animals without affecting basal food intake.

For research and scientific purpose only, not for human use.