BD 1047 dihydrobromide

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Cat.No. 0956 - BD 1047 dihydrobromide | C13H20Cl2N2.2HBr | CAS No. 138356-21-5
Description: σ1 selective antagonist
Chemical Name: N-[2-(3,4-Dichlorophenyl)ethyl]-N-methyl-2-(dimethylamino)ethylamine dihydrobromide
Purity: ≥99% (HPLC)
Datasheet
Citations (23)
Reviews (1)
Literature (1)

Biological Activity

σ1 receptor antagonist, exhibiting a similar binding profile to that of BD 1063 (Cat. No. 0883) but with higher affinity (approximately 10-fold) at both σ1 and σ2 sites.

Compound Libraries

BD 1047 dihydrobromide is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 437.04
Formula C13H20Cl2N2.2HBr
Storage Desiccate at +4°C
Purity ≥99% (HPLC)
CAS Number 138356-21-5
PubChem ID 45073418
InChI Key WOALTFHGLDVJHK-UHFFFAOYSA-N
Smiles Br.Br.CN(C)CCN(C)CCC1=CC=C(Cl)C(Cl)=C1

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 21.85 50
DMSO 21.85 50

Preparing Stock Solutions

The following data is based on the product molecular weight 437.04. 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
0.5 mM 4.58 mL 22.88 mL 45.76 mL
2.5 mM 0.92 mL 4.58 mL 9.15 mL
5 mM 0.46 mL 2.29 mL 4.58 mL
25 mM 0.09 mL 0.46 mL 0.92 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

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

Garrone et al (2000) Effects of traz. on neurotransmitter release from rat mossy fibre cerebellar synaptosomes. Eur.J.Pharmacol. 400 35 PMID: 10913582

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

Romieu et al (2000) Involvement of the sigma1 receptor in the cocaine-induced conditioned place preference. Neuroreport 11 2885 PMID: 11006959


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Keywords: BD 1047 dihydrobromide, BD 1047 dihydrobromide supplier, σ1, sigma1, selective, antagonist, receptors, BD1047, dihydrobromide, Sigma1, Receptors, 0956, Tocris Bioscience

23 Citations for BD 1047 dihydrobromide

Citations are publications that use Tocris products. Selected citations for BD 1047 dihydrobromide include:

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

Gear et al (2014) NOP receptor mediates anti-analgesia induced by agonist-antagonist opioids. Neuroscience 257 139 PMID: 24188792

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

Brailoiu et al (2019) Choline Is an Intracellular Messenger Linking Extracellular Stimuli to IP3-Evoked Ca2+ Signals through Sigma-1 Receptors. Cell Rep 26 330 PMID: 30625315

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. Korean J Physiol Pharmacol 17 1943 PMID: 24485144

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

Su et al (2014) Effects of BD1047, aσ1 receptor antagonist, on the expression of mTOR, Camk2γ and GSK-3β in fluvoxamine-treated N2a cells. Oncotarget 7 435 PMID: 24396420

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

Roh et al (2011) Spinal neuronal NOS activation mediates sigma-1 receptor-induced mechanical and thermal hypersensitivity in mice: involvement of PKC-dependent GluN1 phosphorylation. Br J Pharmacol 163 1707 PMID: 21391983

Yoon et al (2009) Intrathecal injection of the neurosteroid, DHEAS, produces mechanical allodynia in mice: involvement of spinal sigma-1 and GABA receptors. Br J Pharmacol 157 666 PMID: 19422393

Kwon et al (2009) The Antinociceptive Effect of σ-1 Receptor Antagonist, BD1047, in a Capsaicin Induced Headache Model in Rats. Br J Ophthalmol 13 425 PMID: 20054487

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

Moon et al (2014) σ1 receptors activate astrocytes via p38 MAPK phosphorylation leading to the development of mechanical allodynia in a mouse model of neuropathic pain. Br J Pharmacol 171 5881 PMID: 25158784

Lesch et al (2014) Activation and inhibition of transient receptor potential TRPM3-induced gene transcription. Br J Pharmacol 171 2645 PMID: 24895737

Cantarella et al (2007) Protective effects of the σ agonist Pre-084 in the rat retina. Korean J Physiol Pharmacol 91 1382 PMID: 17522150

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

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

Behensky et al (2013) Afobazole activation of σ-1 receptors modulates neuronal responses to amyloid-β25-35. J Pharmacol Exp Ther 347 468 PMID: 24006338

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

Son and Kwon (2010) σ-1 Receptor Antagonist BD1047 Reduces Allodynia and Spinal ERK Phosphorylation Following Chronic Compression of Dorsal Root Ganglion in Rats. J Neurophysiol 14 359 PMID: 21311675

Shin et al (2005) The dextromethorphan analog dimemorfan attenuates kainate-induced seizures via sigma1 receptor activation: comparison with the effects of dextromethorphan. Br J Pharmacol 144 908 PMID: 15723099

Brown et al (2004) Antitussive activity of sigma-1 receptor agonists in the guinea-pig. Br J Pharmacol 141 233 PMID: 14691051


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Reviews for BD 1047 dihydrobromide

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Effect of BD 1047 on viability of 661W cells.
By Timur Mavlyutov on 02/04/2018
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: 661W

MTT (cell viability assay) of 661W cultured cells. Cells were pretreated with sigma-1 receptor antagonist BD 1047. Results show that 100uM concentration of BD1047 significantly inhibited viability of this cell line.

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