BD 1063 dihydrochloride

Pricing Availability   Qty
Description: Selective σ1 ligand, putative antagonist
Chemical Name: 1-[2-(3,4-Dichlorophenyl)ethyl]-4-methylpiperazine dihydrochloride
Purity: ≥99% (HPLC)
Citations (17)
Reviews (2)

Biological Activity for BD 1063 dihydrochloride

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 for BD 1063 dihydrochloride

M. Wt 346.13
Formula C13H18Cl2N2.2HCl
Storage Store at RT
Purity ≥99% (HPLC)
CAS Number 206996-13-6
PubChem ID 11617161
Smiles Cl.Cl.CN1CCN(CCC2=CC=C(Cl)C(Cl)=C2)CC1

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 for BD 1063 dihydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
water 34.61 100

Preparing Stock Solutions for BD 1063 dihydrochloride

The following data is based on the product molecular weight 346.13. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.89 mL 14.45 mL 28.89 mL
5 mM 0.58 mL 2.89 mL 5.78 mL
10 mM 0.29 mL 1.44 mL 2.89 mL
50 mM 0.06 mL 0.29 mL 0.58 mL

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Product Datasheets for BD 1063 dihydrochloride

Certificate of Analysis / Product Datasheet
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References for BD 1063 dihydrochloride

References are publications that support the biological activity of the product.

Liu et al (2005) Cocaine up-regulated fra-2 and σ-1 receptor gene and protein expression in brain regions involved in addiction and reward. J.Pharmacol.Exp.Ther. 314 770 PMID: 15879001

Matsumoto et al (1995) Characterisation of two novel σ receptor ligands: antidystonic effects in rats suggest σ receptor antagonism. Eur.J.Pharmacol. 280 301 PMID: 8566098

McCracken et al (1999) Novel σ receptor ligands attenuate the locomotor stimulatory effects of cocaine. Eur.J.Pharmacol. 365 35 PMID: 9988120

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Keywords: BD 1063 dihydrochloride, BD 1063 dihydrochloride supplier, Selective, σ1, sigma1, ligand, putative, antagonist, Receptors, BD1063, dihydrochloride, Sigma1, 0883, Tocris Bioscience

17 Citations for BD 1063 dihydrochloride

Citations are publications that use Tocris products. Selected citations for BD 1063 dihydrochloride include:

Nguyen et al (2014) Involvement of sigma-1 receptors in the antidepressant-like effects of dextromethorphan. PLoS One 9 e89985 PMID: 24587167

Smith et al (2014) A role for picomolar concentrations of pregnenolone sulfate in synaptic activity-dependent Ca2+ signaling and CREB activation. Mol Pharmacol 86 390 PMID: 25057049

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. Nat Chem Biol 17 1943 PMID: 24485144

Pan et al (2014) σ-1 receptor antagonism restores injury-induced decrease of voltage-gated Ca2+ current in sensory neurons. Oncotarget 350 290 PMID: 24891452

Zhang et al (2013) Methylphenidate enhances NMDA-receptor response in medial prefrontal cortex via sigma-1 receptor: a novel mechanism for methylphen. action. PLoS One 7 e51910 PMID: 23284812

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

Kourrich et al (2013) Dynamic interaction between sigma-1 receptor and Kv1.2 shapes neuronal and behavioral responses to cocaine. Cell 152 236 PMID: 23332758

Cortés-Montero et al (2019) The axonal motor neuropathy-related HINT1 protein is a zinc- and calmodulin-regulated cysteine SUMO protease. Antioxid Redox Signal PMID: 31088288

Rodríguez-Muñoz et al (2015) The ON:OFF switch, σ1R-HINT1 protein, controls GPCR-NMDA receptor cross-regulation: implications in neurological disorders. Int J Neuropsychopharmacol 6 35458 PMID: 26461475

Fishback et al (2012) A 96-well filtration method for radioligand binding analysis of σ receptor ligands. J Pharm Biomed Anal 71 157 PMID: 22910107

Amer et al (2013) Inhibition of endothelial cell Ca2+ entry and transient receptor potential channels by Sigma-1 receptor ligands. Br J Pharmacol 168 1445 PMID: 23121507

Pabba et al (2014) NMDA receptors are upregulated and trafficked to the plasma membrane after sigma-1 receptor activation in the rat hippocampus. J Neurosci 34 11325 PMID: 25143613

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

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

Hiranita et al (2011) Decreases in cocaine self-administration with dual inhibition of the DA transporter and σ receptors. J Pharmacol Exp Ther 339 662 PMID: 21859929

Kurata et al (2004) beta-OE, dehydroepiandrosterone, and dehydroepiandrosterone sulfate protect against N-MthD.-aspartate-induced neurotoxicity in rat hippocampal neurons by different mechanisms. J Pharmacol Exp Ther 311 237 PMID: 15175425

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Reviews for BD 1063 dihydrochloride

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BD1063 binds to sigma-1 receptor.
By Timur Mavlyutov on 02/26/2018
Assay Type: In Vitro
Species: Mouse

We used BD1063 compound as a sigma-1 receptor protector against photolabeling by radioactive iodoazidofenpropimorph in mouse spinal cord homogenate and saw good protective effect with concentration of 10uM.

Use of BD 1063 in mouse brain slices.
By Jordan Yorgason on 01/05/2018
Assay Type: Ex Vivo
Species: Mouse
Cell Line/Tissue: C57

We used BD 1063 as a selective sigma antagonist to test if methamphetamine effects on dopamine release involved sigma receptor activation. BD 1063 (100nM) was applied before methamphetamine treatment. Drug was easy to use, and Tocris' recommendation on concentration for selectivity was useful for the study.

PMID: 29185481 Reference
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