PRE-084 hydrochloride

Catalog # Availability Size / Price Qty
0589/10
0589/50
PRE-084 hydrochloride | CAS No. 138847-85-5 | Sigma1 Receptor Agonists
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Description: Highly selective σ1 agonist

Chemical Name: 2-(4-Morpholinethyl) 1-phenylcyclohexanecarboxylate hydrochloride

Purity: ≥99%

Product Details
Citations (19)
Reviews (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.

Technical Data

M.Wt:
353.89
Formula:
C19H27NO3.HCl
Solubility:
Soluble to 25 mM in water and to 75 mM in DMSO
Purity:
≥99%
Storage:
Store at RT
CAS No:
138847-85-5

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.

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Citations for PRE-084 hydrochloride

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

19 Citations: Showing 1 - 10

  1. The sigma-1 receptor behaves as an atypical auxiliary subunit to modulate the functional characteristics of Kv1.2 channels expressed in HEK293 cells.
    Authors: Abraham Et al.
    Physiol Rep  2019;7:e14147
  2. Choline Is an Intracellular Messenger Linking Extracellular Stimuli to IP3-Evoked Ca2+ Signals through Sigma-1 Receptors.
    Authors: Brailoiu Et al.
    Cell Rep  2019;26:330
  3. Ligands Exert Biased Activity to Regulate Sigma 1 Receptor Interactions With Cationic TRPA1, TRPV1, and TRPM8 Channels.
    Authors: Corté s-Montero Et al.
    Front Pharmacol  2019;10:634
  4. The Sigma-1 Receptor Antagonist, S1RA, Reduces Stroke Damage, Ameliorates Post-Stroke Neurological Deficits and Suppresses the Overexpression of MMP-9.
    Authors: Sánchez-Blázquez Et al.
    Mol Neurobiol  2018;55:4940
  5. Sigma 1 Receptor Antagonists Inhibit Manic-Like Behaviors in Two Congenital Strains of Mice.
    Authors: Sánchez-Blázquez Et al.
    Int J Neuropsychopharmacol  2018;21:938
  6. Cannabidiol enhances MOR antinociception, diminishes NMDA-mediated seizures and reduces stroke damage via the sigma 1 receptor.
    Authors: Rodríguez-Muñoz Et al.
    Mol Brain  2018;11:51
  7. Drug Screening Identifies Sigma-1-Receptor as a Target for the Therapy of VWM Leukodystrophy.
    Authors: Atzmon Et al.
    Front Mol Neurosci  2018;11:336
  8. The ON:OFF switch, σ1R-HINT1 protein, controls GPCR-NMDA receptor cross-regulation: implications in neurological disorders.
    Authors: Rodríguez-Muñoz Et al.
    Br J Pharmacol  2015;6:35458
  9. Orexin-corticotropin-releasing factor receptor heteromers in the ventral tegmental area as targets for cocaine.
    Authors: Navarro Et al.
    Br J Ophthalmol  2015;35:6639
  10. The effects of σ (σ1) receptor-selective ligands on muscarinic receptor antagonist-induced cognitive deficits in mice.
    Authors: Malik Et al.
    Int J Neuropsychopharmacol  2015;172:2519
  11. 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.
    Authors: Szabo Et al.
    PLoS One  2014;9:e106533
  12. Cocaine disrupts histamine H3 receptor modulation of DA D1 receptor signaling: σ1-D1-H3 receptor complexes as key targets for reducing cocaine's effects.
    Authors: Moreno Et al.
    J Neurosci  2014;34:3545
  13. The calcium-sensitive σ-1 receptor prevents cannabinoids from provoking glutamate NMDA receptor hypofunction: implications in antinociception and psychotic diseases.
    Authors: Sánchez-Blázquez Et al.
    J Neurosci  2014;17:1943
  14. Inhibitory effects of sigma-2 receptor agonists on T lymphocyte activation.
    Authors: Iñiguez Et al.
    Front Pharmacol  2013;4:23
  15. Stimulants as specific inducers of DA-independent σ agonist self-administration in rats.
    Authors: Hiranita Et al.
    ScientificWorldJournal  2013;347:42633
  16. Inhibition of tumor cell growth by Sigma1 ligand mediated translational repression.
    Authors: Kim Et al.
    Biochem Biophys Res Commun  2012;426:177
  17. Spinal neuronal NOS activation mediates sigma-1 receptor-induced mechanical and thermal hypersensitivity in mice: involvement of PKC-dependent GluN1 phosphorylation.
    Authors: Roh Et al.
    Br J Pharmacol  2011;163:1707
  18. Protective effects of the σ agonist Pre-084 in the rat retina.
    Authors: Cantarella Et al.
    J Pharmacol Exp Ther  2007;91:1382
  19. Antitussive activity of sigma-1 receptor agonists in the guinea-pig.
    Authors: Brown Et al.
    Br J Pharmacol  2004;141:233

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Worked great for all assays used
By Zeinab Motawe on 05/09/2020
Application: Species: Human

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

PMID: 32279379

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