PRE-084 hydrochloride

Pricing Availability   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)
Citations (19)
Literature (1)

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

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

Solubility Soluble to 25 mM in water and to 75 mM in DMSO


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

If you know of a relevant reference for PRE-084 hydrochloride, please let us know.

View Related Products by Target

View Related Products by Product Action

View all σ1 Receptor Agonists

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

19 Citations for PRE-084 hydrochloride

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

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

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

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

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

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

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

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

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

Do you know of a great paper that uses PRE-084 hydrochloride from Tocris? Please let us know.

Reviews for PRE-084 hydrochloride

There are currently no reviews for this product. Be the first to review PRE-084 hydrochloride and earn rewards!

Have you used PRE-084 hydrochloride?

Submit a review and receive an Amazon gift card.

$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image

$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review

Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

New Product Guide

New Product Guide [Spring/Summer 2019]

Our new product guide highlights over 215 new products added to the Tocris Bioscience range during the first half of 2019.

  • 7-TM Receptors
  • Enzymes
  • Enzyme-Linked Receptors
  • Ion Channels
  • Nuclear Receptors
  • Transporters
  • Chemogenetics
  • Epigenetics
  • Fluorescent Imaging
  • Signal Transduction
  • Stem Cells