PRE-084 hydrochloride

Pricing Availability Delivery Time Qty
Cat.No. 0589 - PRE-084 hydrochloride | C19H27NO3.HCl | CAS No. 138847-85-5
Description: Highly selective σ1 agonist
Chemical Name: 2-(4-Morpholinethyl) 1-phenylcyclohexanecarboxylate hydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations (11)
Literature

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

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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

Safety Datasheet

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


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Keywords: PRE-084 hydrochloride, supplier, selective, σ1, sigma1, agonists, Receptors, cytoprotective, Sigma1, Receptors, Sigma1, Receptors, Tocris Bioscience

11 Citations for PRE-084 hydrochloride

Citations are publications that use Tocris products. Selected citations for PRE-084 hydrochloride include:

Sánchez-Blázquez et al (2014) The calcium-sensitive σ-1 receptor prevents cannabinoids from provoking glutamate NMDA receptor hypofunction: implications in antinociception and psychotic diseases. J Neurosci 17 1943 PMID: 24485144

Iñiguez et al (2013) Inhibitory effects of sigma-2 receptor agonists on T lymphocyte activation. Front Pharmacol 4 23 PMID: 23494519

Hiranita et al (2013) Stimulants as specific inducers of dopamine-independent σ agonist self-administration in rats. ScientificWorldJournal 347 42633 PMID: 23908387

Kim et al (2012) Inhibition of tumor cell growth by Sigma1 ligand mediated translational repression. Biochem Biophys Res Commun 426 177 PMID: 22925888

Cantarella et al (2007) Protective effects of the σ agonist Pre-084 in the rat retina. J Pharmacol Exp Ther 91 1382 PMID: 17522150

Brown et al (2004) Antitussive activity of sigma-1 receptor agonists in the guinea-pig. Br J Pharmacol 141 233 PMID: 14691051

Rodríguez-Muñoz et al (2015) The ON:OFF switch, σ1R-HINT1 protein, controls GPCR-NMDA receptor cross-regulation: implications in neurological disorders. Br J Pharmacol 6 35458 PMID: 26461475

Malik et al (2015) The effects of σ (σ1) receptor-selective ligands on muscarinic receptor antagonist-induced cognitive deficits in mice. Int J Neuropsychopharmacol 172 2519 PMID: 25573298

Navarro et al (2015) Orexin-corticotropin-releasing factor receptor heteromers in the ventral tegmental area as targets for cocaine. Br J Ophthalmol 35 6639 PMID: 25926444

Moreno et al (2014) Cocaine disrupts histamine H3 receptor modulation of dopamine D1 receptor signaling: σ1-D1-H3 receptor complexes as key targets for reducing cocaine's effects. J Neurosci 34 3545 PMID: 24599455

Szabo et al (2014) Psychedelic N,N-dimethyltryptamine and 5-methoxy-N,N-dimethyltryptamine modulate innate and adaptive inflammatory responses through the sigma-1 receptor of human monocyte-derived dendritic cells. PLoS One 9 e106533 PMID: 25171370


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