PRE-084 hydrochloride

Name: PRE-084 hydrochloride
Brand: tocris
SKU: 0589
Rating: 5 (2 reviews)

Catalog # 0589

Citations (19)

(2)

Datasheet / COA / SDS

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Key Product Details

Description:	Highly selective σ₁ agonist
Chemical Name:	2-(4-Morpholinethyl) 1-phenylcyclohexanecarboxylate hydrochloride
Purity:	≥99% (HPLC)
Molecular Weight:	353.89

View Full Technical Details for PRE-084 hydrochloride

Biological Activity

High affinity, selective σ₁ agonist (K_i 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 2.0 Max. 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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	water		25
	DMSO	26.54	75

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 the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.75 mM	3.77 mL	18.84 mL	37.68 mL
3.75 mM	0.75 mL	3.77 mL	7.54 mL
7.5 mM	0.38 mL	1.88 mL	3.77 mL
37.5 mM	0.08 mL	0.38 mL	0.75 mL

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References

References are publications that support the biological activity of the product.

Brown Antitussive activity of sigma-1 receptor agonists in the guinea-pig. Br.J.Pharmacol. 2004 PMID: 14691051
Maurice 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. 1999 PMID: 10385231
Su Sigma compounds derived from phencyclidine. Identification of PRE-084, a new selective sigma ligand. J.Pharmacol.Exp.Ther. 1991 PMID: 1658302
Hyrskyluoto Sigma-1 receptor agonist PRE084 is protective against mutant huntingtin-induced cell degeneration: involvement of calpastatin and the NF-κB pathway. Cell Death Dis. 2013 PMID: 23703391

Citations (19)

Showing 1- 5 of 19 citations Showing All

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

Corté s-Montero et al. (2019) Ligands Exert Biased Activity to Regulate Sigma 1 Receptor Interactions With Cationic TRPA1, TRPV1, and TRPM8 Channels. Front Pharmacol. 10:634
PMID: 31249525
Abraham et al. (2019) The sigma-1 receptor behaves as an atypical auxiliary subunit to modulate the functional characteristics of Kv1.2 channels expressed in HEK293 cells. Physiol Rep. 7:e14147
PMID: 31222975
Brailoiu et al. (2019) Choline Is an Intracellular Messenger Linking Extracellular Stimuli to IP3-Evoked Ca²⁺ Signals through Sigma-1 Receptors. Cell Rep. 26:330
PMID: 30625315
Rodríguez-Muñoz et al. (2018) Cannabidiol enhances MOR antinociception, diminishes NMDA-mediated seizures and reduces stroke damage via the sigma 1 receptor. Mol Brain. 11:51
PMID: 30223868
Sánchez-Blázquez et al. (2018) The Sigma-1 Receptor Antagonist, S1RA, Reduces Stroke Damage, Ameliorates Post-Stroke Neurological Deficits and Suppresses the Overexpression of MMP-9. Mol Neurobiol. 55:4940
PMID: 28779350
Atzmon et al. (2018) Drug Screening Identifies Sigma-1-Receptor as a Target for the Therapy of VWM Leukodystrophy. Front Mol Neurosci. 11:336
PMID: 30279648
Sánchez-Blázquez et al. (2018) Sigma 1 Receptor Antagonists Inhibit Manic-Like Behaviors in Two Congenital Strains of Mice. Int J Neuropsychopharmacol. 21:938
PMID: 29860313
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
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
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
Moreno et al. (2014) Cocaine disrupts histamine H3 receptor modulation of DA D1 receptor signaling: σ1-D1-H3 receptor complexes as key targets for reducing cocaine's effects. J Neurosci. 34:3545
PMID: 24599455
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 DA-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
Roh et al. (2011) Spinal neuronal NOS activation mediates sigma-1 receptor-induced mechanical and thermal hypersensitivity in mice: involvement of PKC-dependent GluN1 phosphorylation. Br J Pharmacol. 163:1707
PMID: 21391983
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

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Showing 1- 5 of 19 citations Showing All

Customer Reviews (2)

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Consistent Reproducible Results

Name: Zeinab Motawe

Species: Human

Assay Type: In Vitro

Cell Line/Tissue: Human Umbilical Vein Endothelial Cells (HUVECs)

I used it to test the effects of sigma-1 receptor activation on glycolysis in endothelial cells using Agilent seahorse XFp instrument (Agilent Technologies, Santa Clara, CA, USA)

PMID: 32279379 Reference
Worked great for all assays used

Name: Zeinab Motawe

Species: Human

Assay Type: In Vitro

Cell Line/Tissue: Human Dermal Microvascular Endothelial Cells (HDMEC)

I used it to test its effect on trans-endothelial electrical resistance (TER) of human dermal microvascular endothelial cells (HDMEC) which gives an idea about endothelial barrier using electrical cell substrate impedance sensing (ECIS). HDMEC (Lifeline cell technologies Frederick, MD, USA) were seeded on ECIS microarrays (applied physics, Troy, NY, USA), grown till confluence. Then cells were serum starved for 1 hour and different concentrations of PRE-084 were added. TER was recorded over time. The graph showed TER differences at 8 hours. n=4/group. Analysis was done by One-Way ANOVA followed by Dunnett's multiple comparison test. *p<0.05. **p<0.005, ***p<0.0005

I diluted it with water and made stock solutions of 10 mM. Stocks were kept in -20.

PMID: 32279379

PRE-084 hydrochloride

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Key Product Details

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Biological Activity

Compound Libraries

Technical Data

Solubility

Preparing Stock Solutions

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Dilution Calculator

Reconstitution Calculator

References

Citations (19)

Customer Reviews (2)

Consistent Reproducible Results

Worked great for all assays used

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