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PD 144418 oxalate

Catalog No. T39211 CAS 1794760-28-3

PD 144418 oxalate is a highly potent and selective sigma 1 (σ1) receptor ligand, displaying a Ki value of 0.08 nM for σ1 and 1377 nM for σ2. It exhibits negligible affinity for other receptors, ion channels, and enzymes. Additionally, PD 144418 oxalate demonstrates potential antipsychotic activity.

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PD 144418 oxalate, CAS 1794760-28-3

Pack Size	Availability	Price/USD
1 mg	In stock	$ 97.00
2 mg	In stock	$ 143.00
5 mg	In stock	$ 248.00
10 mg	In stock	$ 369.00
25 mg	In stock	$ 597.00
50 mg	In stock	$ 865.00
100 mg	In stock	$ 1,160.00
500 mg	In stock	$ 2,330.00

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Purity: 99.08%

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Description	PD 144418 oxalate is a highly potent and selective sigma 1 (σ1) receptor ligand, displaying a Ki value of 0.08 nM for σ1 and 1377 nM for σ2. It exhibits negligible affinity for other receptors, ion channels, and enzymes. Additionally, PD 144418 oxalate demonstrates potential antipsychotic activity.
Targets&IC50	σ2 receptor:1377 nM (Ki), σ1 receptor:0.08 nM (Ki)
In vitro	In vitro, PD 144418 counteracts the increase in cyclic GMP (cGMP) triggered by N-methyl-D-aspartate (NMDA) in rat cerebellar slices, without altering basal levels. This implies a significant role for σ1 sites in controlling actions induced by glutamine. Furthermore, PD 144418 enhances the reduction of 5-hydroxytryptophan induced by Haloperidol within the mesolimbic region, although it does not independently affect 5-HT and dopamine (DA) synthesis [1].
In vivo	Treatment with PD 144418 (10 mg/kg; intraperitoneal injection; male CD-1 mice) effectively antagonized Mescaline-induced scratching without affecting spontaneous motor activity, displaying an ED 50 of 7.0 mg/kg (i.p.). This outcome was observed in a study where male CD-1 mice were administered a single intraperitoneal dose of 10 mg/kg, resulting in the inhibition of scratching behaviors induced by Mescaline.

Molecular Weight	372.42
Formula	C20H24N2O5
CAS No.	1794760-28-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 10 mg/mL (26.85 mM)

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Membrane Protein-targeted Compound Library GPCR Compound Library Bioactive Compounds Library Max Bioactive Compound Library

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Keywords

PD 144418 oxalate 1794760-28-3 GPCR/G Protein Sigma receptor PD 144418 Oxalate PD-144418 Oxalate PD144418 Oxalate inhibitor inhibit

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