PRE-084 hydrochloride

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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 (21)
Reviews (2)

Biological Activity for PRE-084 hydrochloride

PRE-084 hydrochloride is a 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 for PRE-084 hydrochloride

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 for PRE-084 hydrochloride

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 Data for PRE-084 hydrochloride

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

Preparing Stock Solutions for PRE-084 hydrochloride

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.

Select a batch to recalculate based on the batch molecular weight:
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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Product Datasheets for PRE-084 hydrochloride

References for PRE-084 hydrochloride

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

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, PRE-084 hydrochloride supplier, selective, σ1, sigma1, agonists, Receptors, cytoprotective, Sigma1, 0589, Tocris Bioscience

21 Citations for PRE-084 hydrochloride

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

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

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

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

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

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

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

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

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

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

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

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

Song et al (2022) Sigma non-opioid receptor 1 is a potential therapeutic target for long QT syndrome Nat.Cardi.Res. 1 142

Sharma et al (2021) The Sigma-1 receptor is an ER-localized type II membrane protein J Biol Chem 297 101299 PMID: 34648767

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

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

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

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


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Reviews for PRE-084 hydrochloride

Average Rating: 5 (Based on 2 Reviews.)

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Consistent Reproducible Results.
By Zeinab Motawe on 05/19/2020
Assay Type: In Vitro
Species: Human
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.
By Zeinab Motawe on 05/09/2020
Assay Type: In Vitro
Species: Human
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
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