[CAS NO. 138356-21-5] BD-1047dihydrobromide
PRODUCTS SPECIFICATIONS [138356-21-5]
DESCRIPTION [138356-21-5]
Overview
| MDL | MFCD00792739 |
|---|---|
| Molecular Weight | 437.04 |
| Molecular Formula | C13H22Br2Cl2N2 |
| SMILES | CN(C)CCN(CCC1=CC=C(Cl)C(Cl)=C1)C.[H]Br.[H]Br |
3 Publications Citing Use of MCE
Summary
BD-1047 (dihydrobromide) is a selective functional antagonist of sigma-1 receptor , shows antipsychotic activity in animal models predictive of efficacy in schizophrenia [1] .
IC50 & Target
sigma-1 receptor [1]
In Vitro
BD-1047 (dihydrobromide) prevents that Cutamesine reduces the cell death rate induced by light exposure in murine photoreceptor-derived 661w cells
[2]
.
BD-1047 (dihydrobromide) attenuates that Cutamesine reduces the mitochondrial damage and the elevated level of caspase 3/7 activity
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
BD-1047 (dihydrobromide) (1-10 mg/kg; i.p.) decreases the Apomorphine (APO)-induced climbing behavior at the dose of 10 mg/kg in mice
[1]
.
BD-1047 (dihydrobromide) counteracts the antidepressant-like effect induced by co-administration of pramipexole and sertraline (but not pramipexole and fluoxetine)
[3]
.
BD-1047 (dihydrobromide) reduces the increasing expression of pNR1, and reverses the Sig-1 R agonists potentiated NMDA-induced pain behaviour and pNR1 immunoreactivity
[4]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male Albino Swiss mice (50 days old, 25–28 g) [1] |
| Dosage: | 1 mg/kg, 3 mg/kg, 10 mg/kg |
| Administration: | Intraperitoneal injection |
| Result: | Decreased the APO-induced climbing at the dose of 10 mg/kg in mice. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 25 mg/mL ( 57.20 mM ; Need ultrasonic)
H 2 O : 25 mg/mL ( 57.20 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.2881 mL | 11.4406 mL | 22.8812 mL |
| 5 mM | 0.4576 mL | 2.2881 mL | 4.5762 mL |
| 10 mM | 0.2288 mL | 1.1441 mL | 2.2881 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 33.33 mg/mL (76.26 mM); Clear solution; Need ultrasonic
-
2.
-
3.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.72 mM); Clear solution
References
- [1] Skuza G, et al. Effect of BD 1047, a sigma1 receptor antagonist, in the animal models predictive of antipsychotic activity. Pharmacol Rep. 2006 Sep-Oct;58(5):626-635.
- [2] Shimazawa M, et al. Effect of a sigma-1 receptor agonist, cutamesine dihydrochloride (SA4503), on photoreceptor cell death against light-induced damage. Exp Eye Res. 2015 Mar;132:64-72.
- [3] Rogóz Z, et al. Mechanism of synergistic action following co-treatment with pramipexole and fluoxetine or sertraline in the forced swimming test in rats. Pharmacol Rep. 2006 Jul-Aug;58(4):493-500.