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PD 144418

Catalog No. T16445   CAS 154130-99-1

PD 144418 displays potential antipsychotic activity. PD 144418 is a high affinity, potent and selective sigma 1 (σ1) receptor ligand (Ki: 0.08 nM and 1377 nM for σ1 and σ2 respectively). It shows devoid of any significant affinity for other receptors, ion channels, and enzymes.

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PD 144418 Chemical Structure
PD 144418, CAS 154130-99-1
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25 mg 6-8 weeks $ 735.00
50 mg 6-8 weeks $ 955.00
100 mg 6-8 weeks $ 1,440.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description PD 144418 displays potential antipsychotic activity. PD 144418 is a high affinity, potent and selective sigma 1 (σ1) receptor ligand (Ki: 0.08 nM and 1377 nM for σ1 and σ2 respectively). It shows devoid of any significant affinity for other receptors, ion channels, and enzymes.
Targets&IC50 σ2 receptor:1377 nM(ki), σ1 receptor:(ki)0.08 nM
In vitro PD 144418 enhances the reduction in 5-hydroxytryptophan caused by Haloperidol in the mesolimbic region, but by itself has no effect in 5-HT and dopamine (DA) synthesis. PD 144418 reverses the N-methyl-D-aspartate (NMDA)-induced increase in cyclic GMP (cGMP) in rat cerebellar slices without affecting the basal levels, showing that σ1 sites may be important in the regulation of glutamine-induced actions [1].
In vivo PD 144418 has ED50 values is 7.0 mg/kg i.p. 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 [1].
Molecular Weight 282.38
Formula C18H22N2O
CAS No. 154130-99-1

Storage

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

TargetMolReferences 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.

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Keywords

PD 144418 154130-99-1 GPCR/G Protein Sigma receptor PD144418 PD-144418 inhibitor inhibit

 

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