PD 144418 oxalate is a highly potent and selective sigma 1 (σ1) receptor ligand with a Ki value of 0.08 nM for σ1 and 1377 nM for σ2, exhibiting negligible affinity for other receptors, ion channels, and enzymes, and demonstrating potential antipsychotic activity.

σ2 receptor:1377 nM (Ki), σ1 receptor:0.08 nM (Ki)

In vitro, PD 144418 counteracts the increase in cyclic GMP (cGMP) triggered by N-methyl-D-aspartate (NMDA) in rat cerebellar slices, without altering basal levels. This implies a significant role for σ1 sites in controlling actions induced by glutamine. Furthermore, PD 144418 enhances the reduction of 5-hydroxytryptophan induced by Haloperidol within the mesolimbic region, although it does not independently affect 5-HT and dopamine (DA) synthesis [1].

Treatment with PD 144418 (10 mg/kg; intraperitoneal injection; male CD-1 mice) effectively antagonized Mescaline-induced scratching without affecting spontaneous motor activity, displaying an ED 50 of 7.0 mg/kg (i.p.). This outcome was observed in a study where male CD-1 mice were administered a single intraperitoneal dose of 10 mg/kg, resulting in the inhibition of scratching behaviors induced by Mescaline.