PD 144418 oxalate_product_DataBase

Bioactivity	PD 144418 oxalate is a highly affinity, potent and selective sigma 1 (σ1) receptor ligand (Ki 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].
Target	Ki: 0.08 nM (σ1 receptor) and 1377 nM (σ2 receptor)
Invitro	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].
In Vivo	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]. Animal Model:
Name	PD 144418 oxalate
CAS	1794760-28-3
Formula	C20H24N2O5
Molar Mass	372.41
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Reference	[1]. Akunne HC, et al. The pharmacology of the novel and selective sigma ligand, PD 144418. Neuropharmacology. 1997 Jan;36(1):51-62. [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.

PeptideDB

PD 144418 oxalate

CAS: 1794760-28-3 F: C20H24N2O5 W: 372.41