PD 144418 oxalate

Modify Date: 2024-01-12 22:16:54

PD 144418 oxalate Structure
PD 144418 oxalate structure
Common Name PD 144418 oxalate
CAS Number 154130-99-1 Molecular Weight 372.41500
Density N/A Boiling Point N/A
Molecular Formula C18H22N2O Melting Point N/A
MSDS N/A Flash Point N/A

 Use of PD 144418 oxalate


PD 144418 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), devoid of any significant affinity for other receptors, ion channels and enzymes. PD 144418 shows potential antipsychotic activity[1][2].

 Names

Name 3-(4-methylphenyl)-5-(1-propyl-3,6-dihydro-2H-pyridin-5-yl)-1,2-oxazole,oxalic acid
Synonym More Synonyms

 PD 144418 oxalate Biological Activity

Description PD 144418 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), devoid of any significant affinity for other receptors, ion channels and enzymes. PD 144418 shows potential antipsychotic activity[1][2].
Related Catalog
Target

Ki: 0.08 nM (σ1receptor) and 1377 nM (σ2 receptor)[1]

In Vitro 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: Male CD-1 mice induced with Mescaline[1] Dosage: 10 mg/kg Administration: Intraperitoneal injection Result: Antagonized mescaline-induced scratching at doses that did not alter spontaneous motor activity.
References

[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.

 Chemical & Physical Properties

Molecular Formula C18H22N2O
Molecular Weight 372.41500
Exact Mass 372.16900
PSA 103.87000
LogP 3.24260

 Synonyms

PD144418
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