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BD 1047 dihydrobromide

Catalog No.
B6521
σ1 receptor antagonist
Grouped product items
SizePriceStock Qty
10mg
$90.00
In stock
50mg
$330.00
In stock

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Email: [email protected]

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Background

BD 1047 dihydrobromide is an antagonist of σ1 receptor with Ki values of 0.93 and 47 nM for σ-1 receptor and σ-2 receptor, respectively [1].

σ-receptor is a type of opioid receptor. There are two subtypes of σ-receptor: σ-1 and σ-2.σ-1 receptor plays an important role in stimulating dopamine release and modulating the actions of cocaine.

BD 1047 dihydrobromide is a σ-1 receptor antagonist. BD 1047 reduced the dystonia induced by haloperidol and di-o-tolylguanidine (DTG) in a dose-dependent way [1].

In male Wistar rats, BD1047 (20 or 30 mg/kg) reversed response reinstatement induced by the cocaine discriminative stimulus (SD). However, BD1047 had no effect on sweetened condensed milk (SCM) SD-induced responding [2]. In rats with chronic constriction injury (CCI) of the right sciatic nerve, BD1047 significantly relieved CCI-induced mechanical allodynia during the induction. Also, BD1047 significantly increased the expression of σ-1 receptor in the ipsilateral spinal cord dorsal horn and inhibited N-methyl-D-aspartate receptor subunit 1 (NR1) expression and phosphorylation induced by CCI [3].

References:
[1].  Matsumoto RR, Bowen WD, Tom MA, et al. Characterization of two novel sigma receptor ligands: antidystonic effects in rats suggest sigma receptor antagonism. Eur J Pharmacol, 1995, 280(3): 301-310.
[2].  Martin-Fardon R, Maurice T, Aujla H, et al. Differential effects of sigma1 receptor blockade on self-administration and conditioned reinstatement motivated by cocaine vs natural reward. Neuropsychopharmacology, 2007, 32(9): 1967-1973.
[3].  Roh DH, Kim HW, Yoon SY, et al. Intrathecal injection of the sigma(1) receptor antagonist BD1047 blocks both mechanical allodynia and increases in spinal NR1 expression during the induction phase of rodent neuropathic pain. Anesthesiology, 2008, 109(5): 879-889.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt437.04
Cas No.138356-21-5
FormulaC13H20Cl2N2·2HBr
Solubilityinsoluble in ETOH; ≥43.5 mg/mL in H2O with gentle warming; ≥43.9 mg/mL in DMSO with gentle warming
Chemical NameN1-(3,4-dichlorophenethyl)-N1,N2,N2-trimethylethane-1,2-diamine dihydrobromide
SDFDownload SDF
Canonical SMILESClC1=CC(CCN(C)CCN(C)C)=CC=C1Cl.Br.Br
Shipping ConditionShip with blue ice, or upon other requests.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while.

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