1. Neuronal Signaling
  2. Dopamine Transporter
  3. Vanoxerine dihydrochloride

Vanoxerine dihydrochloride (Synonyms: GBR-12909 dihydrochloride; I893 dihydrochloride)

Cat. No.: HY-13217 Purity: 99.52%
Handling Instructions

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.

Vanoxerine dihydrochloride Chemical Structure

Vanoxerine dihydrochloride Chemical Structure

CAS No. : 67469-78-7

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10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
10 mg USD 60 In-stock
Estimated Time of Arrival: December 31
50 mg USD 224 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Vanoxerine dihydrochloride:

Top Publications Citing Use of Products

    Vanoxerine dihydrochloride purchased from MCE. Usage Cited in: Front Cell Neurosci. 2018 Sep 11;12:309.

    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.
    • Biological Activity

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    Description

    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)[1].

    IC50 & Target

    Ki: 1 nM (dopamine reuptake)[1]

    In Vitro

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    In Vivo

    Vanoxerine dihydrochloride (2.5-20 mg/kg; i.p.) significantly increases the ambulatory activity[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Male mice (ddY strain at 6 weeks of age)[3]
    Dosage: 2.5, 5, 10, 20 mg/kg
    Administration: Intraperitoneal injection
    Result: The ambulatory activity of mice increased in a dose-dependent manner, with a maximal increase at 30 min after the administration.
    Clinical Trial
    Molecular Weight

    523.49

    Formula

    C₂₈H₃₄Cl₂F₂N₂O

    CAS No.

    67469-78-7

    SMILES

    FC1=CC=C(C(C2=CC=C(F)C=C2)OCCN3CCN(CCCC4=CC=CC=C4)CC3)C=C1.[2HCl]

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 9.4 mg/mL (17.96 mM; Need ultrasonic and warming)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9103 mL 9.5513 mL 19.1026 mL
    5 mM 0.3821 mL 1.9103 mL 3.8205 mL
    10 mM 0.1910 mL 0.9551 mL 1.9103 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      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

    • 2.

      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

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.08 mg/mL (3.97 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.52%

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    Keywords:

    VanoxerineGBR-12909I893GBR12909GBR 12909I 893I-893Dopamine TransporterDATSLC6A3Inhibitorinhibitorinhibit

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    Product Name:
    Vanoxerine dihydrochloride
    Cat. No.:
    HY-13217
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