Vanoxerine dihydrochloride
Based on 11 publication(s) in Google Scholar
Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) is a competitive, potent, and highly selective dopamine reuptake inhibitor (Ki=1 nM). Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) binds to the target site on the dopamine transporter (DAT).
For research use only. We do not sell to patients.
- Purity: 99.60%
- CAS No.: 67469-78-7
- Formula: C28H34Cl2F2N2O
- Molecular Weight:523.49
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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)
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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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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Publications Citing Use of MedChemExpress (MCE) Vanoxerine dihydrochloride
More- Nature. 2024 Aug;632(8025):686-694. [Abstract]
- Cell. 2025 Nov 26;188(24):6861-6872.e14. [Abstract]
- Nat Commun. 2026 Jun 16. [Abstract]
- Cell Discov. 2026 Apr 28;12(1):30. [Abstract]
- Neuron. 2023 May 17;111(10):1626-1636.e6. [Abstract]
- Transl Psychiatry. 2026 Feb 25;16(1):152. [Abstract]
- Structure. 2026 Jun 8.
- Front Cell Neurosci. 2018 Sep 11:12:309. [Abstract]
- Biochem Biophys Res Commun. 2020 May 14;525(4):989-996. [Abstract]
- bioRxiv. 2024 Dec 23:2024.12.22.629999. [Abstract]
- University of Groningen. 2016 Jun 1.
Customer Validation & Images
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Others
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WB
Biological Activity
Ki: 1 nM (dopamine reuptake)[1]
Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) inhibits the uptake of dopamlne (DA), with an IC50 in the low nanomolar range, and is several-fold less potent as inhibitors of the uptake of noradrenaline and 5-HT[2].
Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) is also an oral, mixed ion channel blocker with IKr, INa, and L-type calcium channel activity[3].
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:Male mice (ddY strain at 6 weeks of age)[3]
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Dosage:2.5, 5, 10, 20 mg/kg
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Administration:Intraperitoneal injection
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Result:The ambulatory activity of mice increased in a dose-dependent manner, with a maximal increase at 30 min after the administration.
Chemical Information
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CAS No. 67469-78-7
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Appearance Solid
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Molecular Weight 523.49
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Formula C28H34Cl2F2N2O
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Color White to off-white
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SMILES
FC1=CC=C(C(C2=CC=C(F)C=C2)OCCN3CCN(CCCC4=CC=CC=C4)CC3)C=C1.[2HCl]
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Synonyms
GBR-12909 dihydrochloride; I893 dihydrochloride
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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 (11)
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Journal Impact Factor
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Most Recent
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Nature
2024 Aug;632(8025):686-694. PMID: 39112701
Vanoxerine dihydrochloride purchased from MedChemExpress. Usage Cited in: Nature. 2024 Aug;632(8025):686-694. [Abstract]
Concentration–inhibition curves of [3H]dopamine uptake by wild-type and indicated mutants of DAT with specified concentrations of GBR12909 (Vanoxerine dihydrochloride) in the range of 1 pM to 10 μM.
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Cell
2025 Nov 26;188(24):6861-6872.e14. PMID: 41138730 -
Nat Commun
Targeting dopamine transporter for treating social transmission of depression-like behaviors in male mice. [Abstract]2026 Jun 16. PMID: 42303982 -
Cell Discov
TGM2-mediated serotonylation of GPX4 confers ferroptosis resistance to promote gastric tumorigenesis. [Abstract]2026 Apr 28;12(1):30. PMID: 42049702 -
Neuron
2023 May 17;111(10):1626-1636.e6. PMID: 36917979 -
Transl Psychiatry
MicroRNA-132/212 negatively modulates opioid reward by targeting dopamine transporter in the ventral tegmental area. [Abstract]2026 Feb 25;16(1):152. PMID: 41741420 -
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Front Cell Neurosci
Differential Regulation of Adhesion and Phagocytosis of Resting and Activated Microglia by Dopamine. [Abstract]2018 Sep 11:12:309. PMID: 30254570
Vanoxerine dihydrochloride purchased from MedChemExpress. Usage Cited in: Front Cell Neurosci. 2018 Sep 11:12:309. [Abstract]
p38MAPK activation by dopamine (DA) can be inhibited by selective DAT blockers (Benztropine and Vanoxerine; 2 μM each) and PMAT blocker (Decynium; 2 μM). Combination of DAT and PMAT blockers further inhibits the activation of p38MAPK.
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Biochem Biophys Res Commun
PGC-1α regulate critical period plasticity via gene × environment interaction in the developmental trajectory to schizophrenia. [Abstract]2020 May 14;525(4):989-996. PMID: 32173526 -
bioRxiv
In vivo multiplex imaging of dynamic neurochemical networks with designed far-red dopamine sensors. [Abstract]2024 Dec 23:2024.12.22.629999. PMID: 39763912 -
Solvent & Solubility
DMSO : 9.4 mg/mL (17.96 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 1 mg/mL (1.91 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: ≥ 2.08 mg/mL (3.97 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (3.97 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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 (273 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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Handling Instructions (2659 KB)
References
[1]. Rothman RB, et al. Dopamine transport inhibitors based on GBR12909 and benztropine as potential medications to treat cocaine addiction. Biochem Pharmacol. 2008 Jan 1;75(1):2-16. [Content Brief]
[2]. Hirate K, et al. Characteristics of the ambulation-increasing effect of GBR-12909, a selective dopamine uptakeinhibitor, in mice. Jpn J Pharmacol. 1991 Apr;55(4):501-11. [Content Brief]
[3]. Andersen PH. The dopamine inhibitor GBR 12909: selectivity and molecular mechanism of action. Eur J Pharmacol. [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 | 1.9103 mL | 9.5513 mL | 19.1026 mL | 47.7564 mL |
| DMSO | 5 mM | 0.3821 mL | 1.9103 mL | 3.8205 mL | 9.5513 mL |
| 10 mM | 0.1910 mL | 0.9551 mL | 1.9103 mL | 4.7756 mL | |
| 15 mM | 0.1274 mL | 0.6368 mL | 1.2735 mL | 3.1838 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.
Vanoxerine dihydrochloride Related Classifications
HY-13217 Related Classifications
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