jnj-31020028

Description: JNJ-31020028 is a potent, selective and brain penetrant small molecule antagonist of the neuropeptide Y(2) receptor with pIC50=8.07 (human); pIC50=8.22 (rat); it is > 100-fold selective versus human Y1/Y4/Y5 receptors. 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.

References: Psychopharmacology (Berl). 2010 Feb; 208(2):265-77; Neuropeptides. 2012 Dec; 46(6):329-34; Alcohol. 2011 Sep; 45(6):567-76.

Related CAS #: 1094873-16-1 (S-isomer); 1094873-14-9 (recemate); 1094873-17-2 (R-isomer);

JNJ 31020028; JNJ-31020028; JNJ31020028;

Chemical Name: N-(4-(4-(2-(diethylamino)-2-oxo-1-phenylethyl)piperazin-1-yl)-3-fluorophenyl)-2-(pyridin-3-yl)benzamide

Exact Mass: 565.2853