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).¹ 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.² 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 β₃-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.

WARNING This product is not for human or veterinary use.

1. Kanatani, A., Ishihara, A., Iwaasa, H., et al. L-152,804: Orally active and selective neuropeptide Y Y5 receptor antagonist. Biochem. Biophys. Res. Commun. 272(1), 169-173 (2000).

2. Mashiko, S., Ishihara, A., Iwaasa, H., et al. A pair-feeding study reveals that a Y5 antagonist causes weight loss in diet-induced obese mice by modulating food intake and energy expenditure. Mol. Pharmacol. 71(2), 602-608 (2007).