PD 144418 displays potential antipsychotic activity. PD 144418 is a high affinity, potent and selective sigma 1 (σ1) receptor ligand (Ki: 0.08 nM and 1377 nM for σ1 and σ2 respectively). It shows devoid of any significant affinity for other receptors, ion channels, and enzymes.

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

PD 144418 enhances the reduction in 5-hydroxytryptophan caused by Haloperidol in the mesolimbic region, but by itself has no effect in 5-HT and dopamine (DA) synthesis. PD 144418 reverses the N-methyl-D-aspartate (NMDA)-induced increase in cyclic GMP (cGMP) in rat cerebellar slices without affecting the basal levels, showing that σ1 sites may be important in the regulation of glutamine-induced actions [1].

PD 144418 has ED50 values is 7.0 mg/kg i.p. PD 144418 (10 mg/kg; intraperitoneal injection; male CD-1 mice) treatment antagonizes Mescaline-induced scratching at doses that did not alter spontaneous motor activity [1].