BD-1008
Based on 1 Customer Validation
BD-1008 is a nonselective σ receptor antagonist with Kis against σ1 receptor and σ2 receptor of 2 nM and 8 nM. The BD-1008 has an extremely low affinity for the D2 receptor (Ki = 1112 nM) and dopamine transporter (DAT) (Ki > 10,000 nM). BD-1008 significantly antagonizes dopamine release in the shell region of the nucleus accumbens via the σ₂ receptor. BD-1008 blocks the self-administration behavior of σ agonists.BD-1008 can be used for the study of addiction therapy that target the σ receptor.
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- Pureté: 98.41%
- CAS No.: 138356-08-8
- Formule: C15H22Cl2N2
- Masse moléculaire:301.25
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Stockage:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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) significantly reduces the self-administration of PRE-084 with an ED50 of 3.45 mg/kg, wdose-dependently blocked PRE-084 self-administration but was inactive against psychoactive substances 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[3]
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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. 138356-08-8
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Appearance Liquid (Density: 1.164±0.06 g/cm3)
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Masse moléculaire 301.25
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Formule C15H22Cl2N2
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Color Colorless to light yellow
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SMILES
CN(CCC1=CC=C(Cl)C(Cl)=C1)CCN2CCCC2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 200 mg/mL (663.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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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| DMSO | 1 mM | 3.3195 mL | 16.5975 mL | 33.1950 mL | 82.9876 mL |
| 5 mM | 0.6639 mL | 3.3195 mL | 6.6390 mL | 16.5975 mL | |
| 10 mM | 0.3320 mL | 1.6598 mL | 3.3195 mL | 8.2988 mL | |
| 15 mM | 0.2213 mL | 1.1065 mL | 2.2130 mL | 5.5325 mL | |
| 20 mM | 0.1660 mL | 0.8299 mL | 1.6598 mL | 4.1494 mL | |
| 25 mM | 0.1328 mL | 0.6639 mL | 1.3278 mL | 3.3195 mL | |
| 30 mM | 0.1107 mL | 0.5533 mL | 1.1065 mL | 2.7663 mL | |
| 40 mM | 0.0830 mL | 0.4149 mL | 0.8299 mL | 2.0747 mL | |
| 50 mM | 0.0664 mL | 0.3320 mL | 0.6639 mL | 1.6598 mL | |
| 60 mM | 0.0553 mL | 0.2766 mL | 0.5533 mL | 1.3831 mL | |
| 80 mM | 0.0415 mL | 0.2075 mL | 0.4149 mL | 1.0373 mL | |
| 100 mM | 0.0332 mL | 0.1660 mL | 0.3320 mL | 0.8299 mL |
BD-1008 Related Classifications
HY-135608 Related Classifications
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