Catalog Number: 0589
Chemical Name: 2-(4-Morpholinethyl) 1-phenylcyclohexanecarboxylate hydrochloride
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. All Tocris products are intended for laboratory research use only.
Background References
  1. Antitussive activity of sigma-1 receptor agonists in the guinea-pig.
    Brown et al.
    Br.J.Pharmacol., 2004;141:233
  2. Sigma compounds derived from phencyclidine. Identification of PRE-084, a new selective sigma ligand.
    Su et al.
    J.Pharmacol.Exp.Ther., 1991;259:543
  3. 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.
    Maurice et al.
    Br.J.Pharmacol., 1999;127:335
  4. Sigma-1 receptor agonist PRE084 is protective against mutant huntingtin-induced cell degeneration: involvement of calpastatin and the NF-κB pathway.
    Hyrskyluoto et al.
    Cell Death Dis., 2013;4:e646
Citations:

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

11 Citations: Showing 1 - 10
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  1. 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
  2. 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
  3. 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
  4. 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
  5. Cocaine disrupts histamine H3 receptor modulation of dopamine 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
  6. 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
  7. Inhibitory effects of sigma-2 receptor agonists on T lymphocyte activation.
    Authors: Iñiguez Et al.
    Front Pharmacol 2013;4:23
  8. Stimulants as specific inducers of dopamine-independent σ agonist self-administration in rats.
    Authors: Hiranita Et al.
    ScientificWorldJournal 2013;347:42633
  9. Inhibition of tumor cell growth by Sigma1 ligand mediated translational repression.
    Authors: Kim Et al.
    Biochem Biophys Res Commun 2012;426:177
  10. Protective effects of the σ agonist Pre-084 in the rat retina.
    Authors: Cantarella Et al.
    J Pharmacol Exp Ther 2007;91:1382
  11. Antitussive activity of sigma-1 receptor agonists in the guinea-pig.
    Authors: Brown Et al.
    Br J Pharmacol 2004;141:233
Expand to show all 11 Citations

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