GBR 12935 dihydrochloride
Based on 1 publication(s) in Google Scholar
GBR 12935 dihydrochloride is a potent, and selective dopamine reuptake inhibitor, with the binding constant (Kd) of 1.08 nM in COS-7 cells. GBR 12935 dihydrochloride stimulates the locomotion activity in different mice strains but fails to induce stereotypy. Thus, GBR 12935 dihydrochloride also prevents the d-Fenfluramine-induced head-twitch response in mice.
For research use only. We do not sell to patients.
- Purity: 99.80%
- CAS No.: 67469-81-2
- Formula: C28H36Cl2N2O
- Molecular Weight:487.50
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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HY-13217
Vanoxerine dihydrochloride
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HY-12242R
GBR 12935 dihydrochloride (Standard)
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HY-13217A
Vanoxerine
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HY-N0480
Reserpine
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HY-12242A
GBR 12935
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HY-13217R
Vanoxerine dihydrochloride (Standard)
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HY-B1124
Fipexide
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HY-N0480R
Reserpine (Standard)
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HY-18332C
DOV-216,303 Free Base
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HY-14560C
Reboxetine mesylate
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HY-18610A
Diclofensine
Publications Citing Use of MedChemExpress (MCE) GBR 12935 dihydrochloride
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Biological Activity
GBR 12909 (10-100 nM) also shows a high affinity for CYP2D6 with the Kd value of 42.2 nM, lower than the affinity for dopamine transporter. The binding effect can be reduced by Quinidine (HY-B1751) and Quinine (HY-D0143), which are the specific and potent inhibitors of CYPZD enzymatic activities[1].
GBR 12935 dihydrochloride (10 nM; 2 min) increases the extracellular levels of dopamine to approximately 400% of basal during the application in the nucleus accumbens[2].
GBR 12935 dihydrochloride (100 μM; 60 min) increases extracellular levels of dopamine compared with levels for artificial cerebrospinal fluid (ACSF) by local perfusion for 60 min[2].
GBR 12935 dihydrochloride (1-9 nM) dose-dependently inhibits active uptake of [3H]dopamine in homogenates of the nucleus accumbens[2].
Co-perfusion of 100 μM GBR 12935 dihydrochloride with either 100 μM Sulpiride (HY-B1019) or Raclopride (HY-103414) produces a significant reduction in the GBR 12935 dihydrochloride induced increase in the extracellular levels of dopamine to basal levels[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult male DBA/2J and C57BL/6J mice (22-30 g)[3]
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Dosage:1.0, 3.2, 10, 32 mg/kg
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Administration:Repeat injection; for 7 days
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Result:Elevated locomotion activity to a greater extent in C57BL/6J mice than DBA/2J mice.
No stereotypy was induced by an eighth day challenge of 10 mg/kg GBR 12935 dihydrochloride in mice pretreated with seven dally injections of either 32 mg/kg cocaine or saline.
Chemical Information
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CAS No. 67469-81-2
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Appearance Solid
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Molecular Weight 487.50
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Formula C28H36Cl2N2O
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Color White to off-white
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SMILES
N1(CCOC(C2=CC=CC=C2)C3=CC=CC=C3)CCN(CCCC4=CC=CC=C4)CC1.Cl.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
Solvent & Solubility
DMSO : 25 mg/mL (51.28 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 7.14 mg/mL (14.65 mM; ultrasonic and warming and heat to 60°C)
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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.13 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.13 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Purity & Documentation
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Data Sheet (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Hiroi T, et al. Specific binding of 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenyl propyl) piperazine (GBR-12935), an inhibitor of the dopamine transporter, to human CYP2D6. Biochem Pharmacol. 1997 Jun 15;53(12):1937-9. [Content Brief]
[2]. Rahman S, et al. Negative interaction of dopamine D2 receptor antagonists and GBR 12909 and GBR 12935 dopamine uptake inhibitors in the nucleus accumbens. Eur J Pharmacol. 2001 Feb 23;414(1):37-44. [Content Brief]
[3]. Tolliver BK, et al. Comparison of cocaine and GBR 12935: effects on locomotor activity and stereotypy in two inbred mouse strains. Pharmacol Biochem Behav. 1994 Jul;48(3):733-9. [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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.0513 mL | 10.2564 mL | 20.5128 mL | 51.2821 mL |
| 5 mM | 0.4103 mL | 2.0513 mL | 4.1026 mL | 10.2564 mL | |
| 10 mM | 0.2051 mL | 1.0256 mL | 2.0513 mL | 5.1282 mL | |
| DMSO | 15 mM | 0.1368 mL | 0.6838 mL | 1.3675 mL | 3.4188 mL |
| 20 mM | 0.1026 mL | 0.5128 mL | 1.0256 mL | 2.5641 mL | |
| 25 mM | 0.0821 mL | 0.4103 mL | 0.8205 mL | 2.0513 mL | |
| 30 mM | 0.0684 mL | 0.3419 mL | 0.6838 mL | 1.7094 mL | |
| 40 mM | 0.0513 mL | 0.2564 mL | 0.5128 mL | 1.2821 mL | |
| 50 mM | 0.0410 mL | 0.2051 mL | 0.4103 mL | 1.0256 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.
GBR 12935 dihydrochloride Related Classifications
HY-12242 Related Classifications
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