BD 1063 dihydrochloride

Name: BD 1063 dihydrochloride
Brand: Tocris Bioscience
SKU: 0883
Rating: 5 (2 reviews)

Tocris Bioscience a Bio-Techne Brand

Catalog # 0883

Citations (17)

(2)

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Key Product Details

Description:	Selective σ₁ ligand, putative antagonist
Chemical Name:	1-[2-(3,4-Dichlorophenyl)ethyl]-4-methylpiperazine dihydrochloride
Purity:	≥99% (HPLC)
Molecular Weight:	346.13

View Full Technical Details for BD 1063 dihydrochloride

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
InChi Key	NXFDBTLQOARIMH-UHFFFAOYSA-N
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 for BD 1063 dihydrochloride

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	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.

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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References for BD 1063 dihydrochloride

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

Liu 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. 2005 PMID: 15879001
McCracken Novel σ receptor ligands attenuate the locomotor stimulatory effects of cocaine. Eur.J.Pharmacol. 1999 PMID: 9988120
Matsumoto Characterisation of two novel σ receptor ligands: antidystonic effects in rats suggest σ receptor antagonism. Eur.J.Pharmacol. 1995 PMID: 8566098

Citations for BD 1063 dihydrochloride (17)

Showing 1 - 10 of 17 citations Showing All

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Citations are publications that use Bio-Techne products. Selected citations for BD 1063 dihydrochloride include:

Cortés-Montero et al. (2019) The axonal motor neuropathy-related HINT1 protein is a zinc- and calmodulin-regulated cysteine SUMO protease. Antioxid Redox Signal. 2019;
PMID: 31088288
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
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
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
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
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
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
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
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
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
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
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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BD1063 binds to sigma-1 receptor

Name: Timur Mavlyutov

Species: Mouse

Assay Type: In Vitro

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

Name: Jordan Yorgason

Species: Mouse

Assay Type: Ex Vivo

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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