Potent and selective galanin receptor 2 (GAL2) agonist (EC50 = 38 nM, Ki values are 6.55, 497 and 587 nM at GAL2, GAL3 and GAL1 respectively). Has an additive effect on the signal transduction of galanin.

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.

Galanin (1-30), human is a 30-amino acid neuropeptide, and acts as an agonist of GalR1 and GalR2 receptors, with Kis of both 1 nM. Endogenous peptide with multiple endocrine, metabolic and behavioral effects. Has been shown to have an action on intestinal smooth muscle, insulin and somatostatin release, and synaptic neurotransmission.