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BD 1063 dihydrochloride
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.
|Storage||Store at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
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|
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
16 Citations for BD 1063 dihydrochloride
Citations are publications that use Tocris products. Selected citations for BD 1063 dihydrochloride include:
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
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
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
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
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
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
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
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
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Reviews for BD 1063 dihydrochloride
Average Rating: 5 (Based on 2 Reviews.)
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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.
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.
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