BD-1008 dihydrobromide
Based on 1 Customer Validation
BD-1008 dihydrobromide is a nonselective σ receptor antagonist with Kis against σ1 receptor and σ2 receptor of 2 nM and 8 nM. The BD-1008 dihydrobromide has an extremely low affinity for the D2 receptor (Ki = 1112 nM) and dopamine transporter (DAT) (Ki > 10,000 nM). BD-1008 dihydrobromide significantly antagonizes dopamine release in the shell region of the nucleus accumbens via the σ₂ receptor. BD-1008 dihydrobromide blocks the self-administration behavior of σ agonists.BD-1008 dihydrobromide can be used for the study of addiction therapy that target the σ receptor.
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- Pureté : 98.07%
- CAS No.: 138356-09-9
- Formule: C15H24Br2Cl2N2
- Masse moléculaire:463.08
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
σ1 2 nM (Ki) |
σ2 8 nM (Ki) |
In Vivo
BD-1008 (1-10 mg/kg, i.p., after multiple doses) dihydrobromide significantly reduces the self-administration of PRE-084 with an ED50 of 3.45 mg/kg in rats[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Self-Administration experiment established in male Sprague–Dawley rats, weighing 300 g[1]
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Dosage:0.03, 0.10, 0.32, and 1.0 mg/kg per injection
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Administration:Intraperitoneal injection (i.p.), achieved 1-10 mg/kg after multiple administrations
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Result:Dose-dependently blocked PRE-084 self-administration but was inactive against d-methamphetamine, heroin, and ketamine.
Chemical Information
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CAS No. 138356-09-9
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Appearance Solid
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Masse moléculaire 463.08
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Formule C15H24Br2Cl2N2
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Color White to off-white
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SMILES
CN(CCC1=CC=C(Cl)C(Cl)=C1)CCN2CCCC2.Br.Br
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 50 mg/mL (107.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 12.5 mg/mL (26.99 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (273 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Staelens L, et al. In vivo evaluation of [(123)I]-3-(4-iodobenzyl)-1,2,3,4-tetrahydro-8-hydroxychromeno[3,4-c]pyridin-5-one: a presumed dopamine D4 receptor ligand for SPECT studies. Nucl Med Biol. 2005 Apr;32(3):293-9. [Content Brief]
[2]. Garcés-Ramírez L, et al. Sigma receptor agonists: receptor binding and effects on mesolimbic dopamine neurotransmission assessed by microdialysis. Biol Psychiatry. 2011 Feb 1;69(3):208-17. [Content Brief]
[3]. Hiranita T, et al. Stimulants as specific inducers of dopamine-independent σ agonist self-administration in rats. J Pharmacol Exp Ther. 2013 Oct;347(1):20-9. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| H2O / DMSO | 1 mM | 2.1595 mL | 10.7973 mL | 21.5945 mL | 53.9864 mL |
| 5 mM | 0.4319 mL | 2.1595 mL | 4.3189 mL | 10.7973 mL | |
| 10 mM | 0.2159 mL | 1.0797 mL | 2.1595 mL | 5.3986 mL | |
| 15 mM | 0.1440 mL | 0.7198 mL | 1.4396 mL | 3.5991 mL | |
| 20 mM | 0.1080 mL | 0.5399 mL | 1.0797 mL | 2.6993 mL | |
| 25 mM | 0.0864 mL | 0.4319 mL | 0.8638 mL | 2.1595 mL | |
| DMSO | 30 mM | 0.0720 mL | 0.3599 mL | 0.7198 mL | 1.7995 mL |
| 40 mM | 0.0540 mL | 0.2699 mL | 0.5399 mL | 1.3497 mL | |
| 50 mM | 0.0432 mL | 0.2159 mL | 0.4319 mL | 1.0797 mL | |
| 60 mM | 0.0360 mL | 0.1800 mL | 0.3599 mL | 0.8998 mL | |
| 80 mM | 0.0270 mL | 0.1350 mL | 0.2699 mL | 0.6748 mL | |
| 100 mM | 0.0216 mL | 0.1080 mL | 0.2159 mL | 0.5399 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
BD-1008 dihydrobromide Related Classifications
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