IC50: 17.4 nM (σ1receptor, guinea pig brain membranes)

The sigma receptor might be involved in several diseases in the central nervous system. Cutamesine, a potent σ1receptor agonist, has 103-fold higher affinity for σ1 (IC ₅₀ =17.4 nM) than σ2 (IC ₅₀ =1,784 nM) sites in guinea pig brain membranes. Cutamesine is 14-fold selective for σ1 (K _i =4.6 nM) over σ2 (K _i =63.1 nM) sites in guinea pig brain homogenates. Cutamesine protects motor neuron NSC34 cells against superoxide dismutase 1 and serum free neurotoxicity. It upregulates the phosphorylation levels of Akt and extracellular signal-regulated kinase (ERK) 1/2. Cutamesine reduces the activation of the MAPK/ERK pathway and down-regulated the ionotropic glutamate receptor, GluR1.

Cutamesine extends the survival time in the SOD1G93A mice.