A new protocol for evaluating novel GPCR ligands using real-time impedance based technology showed similar or slightly lower EC₅₀ values when compared to previously published galanin ligands

M1154, a novel GAL_1/2R selective agonist was designed and its ability to significantly reduce the excitotoxicity of i.c.v. administered KA was evaluated.

Our data indicate, that M617 (GAL₁R selective ligand) and M1154 (GAL_1/2R selective ligand), but not M1145 (GAL₂R selective ligand), significantly reduced neuronal cell death, in the KA-excitoxicity model.

Our findings suggest that the neuroprotective effect of pharmacological stimulation of galanin receptors in vivo after I.c.v. administration of KA in the CA3 region is mediated through GAL₁R.