L-152,804

L-152,804 is an antagonist of neuropeptide Y (NPY) receptor Y5 (IC50s = 26 and 31 nM for the human and rat receptors, respectively). It is selective for Y5 over Y1, Y2, and Y4 receptors (IC50s = >10,000 nM for the human receptors). L-152,804 (30 µg, i.c.v.) reduces bovine pancreatic peptide-induced, but not NPY-induced, food intake in satiated rats. It reduces body weight in diet-induced obese (DIO) mice to a greater extent than pair-fed DIO mice without reducing food intake when administered at a dose of 100 mg/kg. It also reduces mesenteric adipose tissue weight in DIO mice when compared to pair-fed DIO or ad libitum-fed DIO mice and reduces hepatic triglyceride levels in DIO mice when compared to ad libitum-fed DIO mice. L-152,804 increases expression of the genes encoding mitochondrial uncoupling protein 1 (UCP1) and UCP3 in brown adipose tissue (BAT) and the beta3-adrenergic receptor in white adipose tissue (WAT) of DIO mice compared to pair-fed and ad libitum-fed DIO mice. It does not increase energy expenditure in DIO mice compared to lean mice.. Solulibility: DMSO: Slightly Soluble: 0.1-1 mg/ml: Ethanol: Slightly Soluble: 0.1-1 mg/ml.