Neuropeptide FF receptor agonist (Ki values are 48.4 and 12.1 nM for NPFF1 and NPFF2, respectively). Potentiates the antinociceptive action of morphine in vivo and reverses the loss of morphine potency in tolerant animals. Also increases the amplitude of the sustained current of heterologously expressed acid sensing ion channel 3 (ASIC3) (EC50 ~ 50 μM).

Cocaine- and amphetamine-regulated transcript (CART) with potent appetite-suppressing activity. Satiety factor; inhibits normal and starvation-induced feeding. Closely related to the actions of leptin and neuropeptide Y; blocks the neuropeptide Y-induced feeding response. Induces anxiety and stress behavior in rodents.

Potent neuropeptide Y (NPY) Y5 receptor agonist (pEC50 values are 7.82, 6.28, 6.44 and > 6 at rat Y5, Y4, Y1 and Y2 receptors respectively) that displays > 26-fold, > 1000-fold and > 1000-fold selectivity over Y1, Y2 and Y4 receptors respectively. Induces hyperphagia, body weight gain, adiposity, hypercholesterolemia, hyperinsulinemia and hyperleptinemia in vivo. Orally active.