Biological Activity
High affinity, selective σ1 ligand (Ki values are 0.08 and 1377 nM for σ1 and σ2 respectively). Displays no significant activity at a wide range of other receptors, ion channels and enzymes. Antagonizes mescaline-induced scratching in mice following i.p. administration. Also attenuates cocaine-induced hyperactivity in mice.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Technical Data
| M. Wt | 372.42 |
| Formula | C18H22N2O.C2H2O4 |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 154130-99-1 |
| PubChem ID | 9817231 |
| InChI Key | FOQRKFCLRMMKAT-UHFFFAOYSA-N |
| Smiles | O=C(O)C(O)=O.CCCN1CC(C2=CC(C3=CC=C(C)C=C3)=NO2)=CCC1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 18.62 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 372.42. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.69 mL | 13.43 mL | 26.85 mL |
| 5 mM | 0.54 mL | 2.69 mL | 5.37 mL |
| 10 mM | 0.27 mL | 1.34 mL | 2.69 mL |
| 50 mM | 0.05 mL | 0.27 mL | 0.54 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Akunne et al (1997) The pharmacology of the novel and selective sigma ligand, PD 144418. Neuropharmacology 36 51 PMID: 9144641
Lever et al (2014) Relationship between cerebral sigma-1 receptor occupancy and attenuation of cocaine's motor stimulatory effects in mice by PD144418. J.Pharmacol.Exp.Ther. 351 153 PMID: 25100754
Keywords: PD 144418 oxalate, supplier, High, affinity, selective, σ1, sigma1, ligands, Receptors, PD144418, oxalate, Pfizer, Sigma1, Receptors, Sigma1, Receptors, Tocris Bioscience
