1. Neuronal Signaling
  2. Dopamine Transporter
  3. Vanoxerine

Vanoxerine (GBR-12909) is a competitive, potent, and highly selective dopamine reuptake inhibitor (Ki=1 nM). Vanoxerine (GBR-12909) binds to the target site on the dopamine transporter (DAT).

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Vanoxerine dihydrochloride) usually boasts enhanced water solubility and stability.

For research use only. We do not sell to patients.

Vanoxerine Chemical Structure

Vanoxerine Chemical Structure

CAS No. : 67469-69-6

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Top Publications Citing Use of Products

    Vanoxerine 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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    Description

    Vanoxerine (GBR-12909) is a competitive, potent, and highly selective dopamine reuptake inhibitor (Ki=1 nM). Vanoxerine (GBR-12909) binds to the target site on the dopamine transporter (DAT)[1].

    IC50 & Target

    Ki: 1 nM (dopamine reuptake)[1]

    In Vitro

    Vanoxerine (GBR-12909) 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 (GBR-12909) 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.

    In Vivo

    Vanoxerine (GBR-12909) (2.5-20 mg/kg; i.p.) significantly increases the ambulatory activity[3].

    MedChemExpress (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

    450.56

    Formula

    C28H32F2N2O

    CAS No.
    SMILES

    FC1=CC=C(C(C2=CC=C(F)C=C2)OCCN3CCN(CCCC4=CC=CC=C4)CC3)C=C1

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    Purity & Documentation
    References
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    Vanoxerine Related Classifications

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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