BD 1063 dihydrochloride
1 Image
Description: Selective σ1 ligand, putative antagonist
Chemical Name: 1-[2-(3,4-Dichlorophenyl)ethyl]-4-methylpiperazine dihydrochloride
Purity: ≥99%
Biological Activity
BD 1063 dihydrochloride is a 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Sigma receptor ligand, (+)-pentazocine, suppresses inflammatory responses of retinal microglia.
Zhao J, Ha Y, Liou G, Gonsalvez G, Smith S, Bollinger K
Invest Ophthalmol Vis Sci, 2014;55(6):3375-84. -
High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
Fox JT, Sakamuru S, Huang R
Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8. -
Novel σ receptor ligands attenuate the locomotor stimulatory effects of cocaine.
McCracken et al.
Eur.J.Pharmacol., 1999;365:35 -
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 -
Characterisation of two novel σ receptor ligands: antidystonic effects in rats suggest σ receptor antagonism.
Matsumoto et al.
Eur.J.Pharmacol., 1995;280:301
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Citations for BD 1063 dihydrochloride
The citations listed below are publications that use Tocris products. Selected citations for BD 1063 dihydrochloride include:
17 Citations: Showing 1 - 10
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The axonal motor neuropathy-related HINT1 protein is a zinc- and calmodulin-regulated cysteine SUMO protease.
Authors: Cortés-Montero Et al.
Antioxid Redox Signal 2019;
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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
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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
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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
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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
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Involvement of sigma-1 receptors in the antidepressant-like effects of dextromethorphan.
Authors: Nguyen Et al.
PLoS One 2014;9:e89985
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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
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σ-1 receptor antagonism restores injury-induced decrease of voltage-gated Ca2+ current in sensory neurons.
Authors: Pan Et al.
Oncotarget 2014;350:290
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NMDA receptors are upregulated and trafficked to the plasma membrane after sigma-1 receptor activation in the rat hippocampus.
Authors: Pabba Et al.
J Neurosci 2014;34:11325
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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
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Methylphenidate enhances NMDA-receptor response in medial prefrontal cortex via sigma-1 receptor: a novel mechanism for methylphen. action.
Authors: Zhang Et al.
PLoS One 2013;7:e51910
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Inhibitory effects of sigma-2 receptor agonists on T lymphocyte activation.
Authors: Iñiguez Et al.
Front Pharmacol 2013;4:23
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Inhibition of endothelial cell Ca2+ entry and transient receptor potential channels by Sigma-1 receptor ligands.
Authors: Amer Et al.
Br J Pharmacol 2013;168:1445
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Dynamic interaction between sigma-1 receptor and Kv1.2 shapes neuronal and behavioral responses to cocaine.
Authors: Kourrich Et al.
Cell 2013;152:236
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A 96-well filtration method for radioligand binding analysis of σ receptor ligands.
Authors: Fishback Et al.
J Pharm Biomed Anal 2012;71:157
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Decreases in cocaine self-administration with dual inhibition of the DA transporter and σ receptors.
Authors: Hiranita Et al.
J Pharmacol Exp Ther 2011;339:662
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beta-OE, dehydroepiandrosterone, and dehydroepiandrosterone sulfate protect against N-MthD.-aspartate-induced neurotoxicity in rat hippocampal neurons by different mechanisms.
Authors: Kurata Et al.
J Pharmacol Exp Ther 2004;311:237
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