Biological Activity
High affinity, selective σ1 agonist (Ki values are 2.2 and 13091 nM for σ1 and σ2 receptors respectively). Selective over PCP receptors (IC50 > 100000 nM) and several other receptor systems. Produces antiamnesic and antitussive effects in vivo. Also exhibits protective effects in PC6.3 cells expressing mutant huntingtin by activating NF-κB signaling.
Compound Libraries
PRE-084 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 353.89 |
| Formula | C19H27NO3.HCl |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 138847-85-5 |
| PubChem ID | 11314197 |
| InChI Key | QUJWFJNHTBKCLU-UHFFFAOYSA-N |
| Smiles | Cl.O=C(OCCN1CCOCC1)C1(CCCCC1)C1=CC=CC=C1 |
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 | 26.54 | 75 | |
| water | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 353.89. 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 | 2.83 mL | 14.13 mL | 28.26 mL |
| 5 mM | 0.57 mL | 2.83 mL | 5.65 mL |
| 10 mM | 0.28 mL | 1.41 mL | 2.83 mL |
| 50 mM | 0.06 mL | 0.28 mL | 0.57 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Brown et al (2004) Antitussive activity of sigma-1 receptor agonists in the guinea-pig. Br.J.Pharmacol. 141 233 PMID: 14691051
Maurice et al (1999) The attenuation of learning impairments induced after exposure to CO or trimethyltin in mice by sigma (σ) receptor ligands involves both σ1 and σ2 sites. Br.J.Pharmacol. 127 335 PMID: 10385231
Su et al (1991) Sigma compounds derived from phencyclidine. Identification of PRE-084, a new selective sigma ligand. J.Pharmacol.Exp.Ther. 259 543 PMID: 1658302
Hyrskyluoto et al (2013) Sigma-1 receptor agonist PRE084 is protective against mutant huntingtin-induced cell degeneration: involvement of calpastatin and the NF-κB pathway. Cell Death Dis. 4 e646 PMID: 23703391
Keywords: PRE-084 hydrochloride, supplier, selective, σ1, sigma1, agonists, Receptors, cytoprotective, Sigma1, Receptors, Sigma1, Receptors, Tocris Bioscience
