PD 144418 oxalate is a highly affinity, potent and selectivesigma 1 (σ1) receptorligand (K_ivalues of 0.08 nM and 1377 nM forσ1and σ2 respectively). PD 144418 oxalate devoids of any significant affinity for other receptors, ion channels and enzymes. PD 144418 oxalate shows potential antipsychotic activity^[1][2].

Ki: 0.08 nM (σ1 receptor) and 1377 nM (σ2 receptor)^[1]

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

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, with PD 144418 showing ED₅₀values of 7.0 mg/kg i.p.^[1].

372.41

Solid

C₂₀H₂₄N₂O₅

1794760-28-3

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)