BD 1047 dihydrobromideσ1 receptor antagonist CAS# 138356-21-5 |
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Quality Control & MSDS
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| Cas No. | 138356-21-5 | SDF | Download SDF |
| PubChem ID | 45073418 | Appearance | Powder |
| Formula | C13H22Br2Cl2N2 | M.Wt | 437.04 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 25 mg/mL (57.20 mM; Need ultrasonic) | ||
| Chemical Name | N'-[2-(3,4-dichlorophenyl)ethyl]-N,N,N'-trimethylethane-1,2-diamine;dihydrobromide | ||
| SMILES | CN(C)CCN(C)CCC1=CC(=C(C=C1)Cl)Cl.Br.Br | ||
| Standard InChIKey | WOALTFHGLDVJHK-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C13H20Cl2N2.2BrH/c1-16(2)8-9-17(3)7-6-11-4-5-12(14)13(15)10-11;;/h4-5,10H,6-9H2,1-3H3;2*1H | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | σ1 receptor antagonist, exhibiting a similar binding profile to that of BD 1063 but with higher affinity (approximately 10-fold) at both σ1 and σ2 sites. |
BD 1047 dihydrobromide Dilution Calculator
BD 1047 dihydrobromide Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.2881 mL | 11.4406 mL | 22.8812 mL | 45.7624 mL | 57.203 mL |
| 5 mM | 0.4576 mL | 2.2881 mL | 4.5762 mL | 9.1525 mL | 11.4406 mL |
| 10 mM | 0.2288 mL | 1.1441 mL | 2.2881 mL | 4.5762 mL | 5.7203 mL |
| 50 mM | 0.0458 mL | 0.2288 mL | 0.4576 mL | 0.9152 mL | 1.1441 mL |
| 100 mM | 0.0229 mL | 0.1144 mL | 0.2288 mL | 0.4576 mL | 0.572 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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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.
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Effects of trazodone on neurotransmitter release from rat mossy fibre cerebellar synaptosomes.[Pubmed:10913582]
Eur J Pharmacol. 2000 Jul 14;400(1):35-41.
The effects of trazodone and putative sigma (sigma) receptor ligands were investigated on KCl-stimulated release of glutamate (Glu) and gamma-aminobutyric acid (GABA) from cerebellar mossy fibre synaptosomes. Both trazodone and serotonin (5-HT) inhibited the increase of Glu and GABA release evoked by 15 mM KCl. Trazodone increased the inhibition of Glu release caused by 0.01 microM 5-HT, while it antagonized the inhibition induced by higher 5-HT concentrations. Despite the low affinity of trazodone for both sigma(1) and sigma(2) binding sites, with a pK(i) of 5.9 and 6.0 respectively, two sigma receptor ligands, (+)-3-[3-hydroxypheny]-N-(1-propyl)piperidine ((+)-3-PPP) and N-[2-(3,4-dichlorophenyl)ethyl]-N-methyl-2-(dimethylamino)ethylamine (BD 1047) antagonized the effects of trazodone. The putative sigma receptor ligand N-allylnormetazocine ((+)-SKF 10,047) mimicked the inhibitory effect of trazodone. As with trazodone, (+)-3-PPP and BD 1047 antagonized the activity of (+)-SKF 10,047 but not that of 5-HT. On the whole, these results suggest that trazodone shares a common molecular target with sigma compounds distinct from that of 5-HT and is involved in K(+)-stimulated Glu and GABA release from mossy fibre cerebellar synaptosomes.
Involvement of the sigma1 receptor in the cocaine-induced conditioned place preference.[Pubmed:11006959]
Neuroreport. 2000 Sep 11;11(13):2885-8.
The sigma1 (sigma1) receptor constitutes a particular target of cocaine believed to be involved in some of its behavioral effects. In the present study, its involvement in the rewarding effect of cocaine was examined using the conditioned place preference (CPP) procedure. CPP was induced in C57Bl/6 mice injected repeatedly with cocaine (20 mg/kg, i.p.). The selective sigma1 receptor antagonists NE-100 and BD1047 (1-10 mg/kg, i.p.) significantly attenuated or blocked the cocaine-induced CPP. Animals treated centrally with a sigma1 receptor antisense oligodeoxynucleotide failed to develop cocaine-induced CPP, unlike mismatch controls. The sigma1 receptor thus appears to be critically involved in the development of the cocaine-induced CPP and, in consequence, may constitute a promising approach to blocking cocaine reward.
Characterization of two novel sigma receptor ligands: antidystonic effects in rats suggest sigma receptor antagonism.[Pubmed:8566098]
Eur J Pharmacol. 1995 Jul 14;280(3):301-10.
The novel sigma receptor ligands, N(-)[2-(3,4-dichlorophenyl)ethyl]-N-methyl-2-(dimethylamino)ethylamine (BD1047) and 1(-)[2-(3,4-dichlorophenyl)ethyl]-4-methylpiperazine (BD1063), were characterized in rats using binding assays and behavioral studies. In radioligand binding studies, the novel ligands showed marked selectivity for sigma binding sites, generally having a 100-fold or better affinity for sigma sites compared to nine other tested receptors (opiate, phencyclidine, muscarinic, dopamine, alpha 1-, alpha 2-, beta-adrenoceptor, 5-HT1, 5-HT2); the only exception was the affinity of BD1047 for beta-adrenoceptors. Competition assays further revealed that the drugs interacted with both sigma 1 and sigma 2 binding sites. Although both drugs had preferential affinities for sigma 1 sites, BD1047 exhibited a higher affinity for sigma 2 sites than BD1063. In behavioral studies, BD1047 and BD1063 had no effects on their own when unilaterally microinjected into the red nucleus of rats, but both compounds attenuated the dystonia produced by the high affinity sigma ligands, di-o-tolylguanidine (DTG) and haloperidol. BD1047 and BD1063 dose-dependently attenuated the dystonia produced by DTG, suggesting a receptor-mediated mechanism, and the dose curve for DTG was shifted to the right in the presence of the novel ligands. BD1047 and BD1063 appear to act as antagonists at sigma sites and may represent promising new tools for probing other functional effects associated with sigma binding sites.
