PD 144418 oxalate 

PD 144418 oxalate is a highly affinity, potent and selective sigma 1 (σ1) receptor ligand (K_i values of 0.08 nM and 1377 nM for σ1 and 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 ED₅₀ values of 7.0 mg/kg i.p.^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

372.41

C₂₀H₂₄N₂O₅

1794760-28-3

固体

White to off-white

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)

• [1]. Akunne HC, et al. The pharmacology of the novel and selective sigma ligand, PD 144418. Neuropharmacology. 1997 Jan;36(1):51-62.  [Content Brief]

  [2]. Lever JR, et al. Relationship between cerebral sigma-1 receptor occupancy and attenuation of cocaine's motor stimulatory effects in mice by PD144418. J Pharmacol Exp Ther. 2014 Oct;351(1):153-63.  [Content Brief]