Catalog Number: 0883
Chemical Name: 1-[2-(3,4-Dichlorophenyl)ethyl]-4-methylpiperazine dihydrochloride
Biological Activity
σ1 receptor antagonist, approximately 50-fold selective over σ2 sites and ≥100-fold selective over opioid, PCP, muscarinic, dopamine, α1, α2, β adrenoceptor, 5-HT1 and 5-HT2 receptors. Prevents hyperlocomotion following cocaine administration in mice.
Technical Data
  • M.Wt:
    346.13
  • Formula:
    C13H18Cl2N2.2HCl
  • Solubility:
    Soluble to 100 mM in water
  • Purity:
    >99%
  • Storage:
    Store at RT
  • CAS No:
    206996-13-6
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. Novel σ receptor ligands attenuate the locomotor stimulatory effects of cocaine.
    McCracken et al.
    Eur.J.Pharmacol., 1999;365:35
  2. Cocaine up-regulated fra-2 and σ-1 receptor gene and protein expression in brain regions involved in addiction and reward.
    Liu et al.
    J.Pharmacol.Exp.Ther., 2005;314:770
  3. Characterisation of two novel σ receptor ligands: antidystonic effects in rats suggest σ receptor antagonism.
    Matsumoto et al.
    Eur.J.Pharmacol., 1995;280:301
Citations:

The citations listed below are publications that use Tocris products. Selected citations for BD 1063 dihydrochloride include:

9 Citations: Showing 1 - 9
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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.
    Int J Neuropsychopharmacol 2015;6:35458
  2. Involvement of sigma-1 receptors in the antidepressant-like effects of dextromethorphan.
    Authors: Nguyen Et al.
    PLoS One 2014;9:e89985
  3. A role for picomolar concentrations of pregnenolone sulfate in synaptic activity-dependent Ca2+ signaling and CREB activation.
    Authors: Smith Et al.
    Mol Pharmacol 2014;86:390
  4. σ-1 receptor antagonism restores injury-induced decrease of voltage-gated Ca2+ current in sensory neurons.
    Authors: Pan Et al.
    Oncotarget 2014;350:290
  5. 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.
    Nat Chem Biol 2014;17:1943
  6. Methylphenidate enhances NMDA-receptor response in medial prefrontal cortex via sigma-1 receptor: a novel mechanism for methylphenidate action.
    Authors: Zhang Et al.
    PLoS One 2013;7:e51910
  7. Inhibitory effects of sigma-2 receptor agonists on T lymphocyte activation.
    Authors: Iñiguez Et al.
    Front Pharmacol 2013;4:23
  8. Dynamic interaction between sigma-1 receptor and Kv1.2 shapes neuronal and behavioral responses to cocaine.
    Authors: Kourrich Et al.
    Cell 2013;152:236
  9. Decreases in cocaine self-administration with dual inhibition of the dopamine transporter and σ receptors.
    Authors: Hiranita Et al.
    J Pharmacol Exp Ther 2011;339:662

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