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).

Velneperit is potent and selective neuropeptide Y (NPY) Y5 receptor under evaluating for treatment of obesity.

Potent endogenous neuropeptide S receptor (NPSR) agonist (EC50 = 3 nM). Induces mobilization of intracellular Ca2+. Increases locomotor activity and wakefulness in mice. Also reduces anxiety-like behavior in mice.