VanoxerineVanoxerine
MedChemExpress (MCE)
HY-13217A
67469-69-6
GBR 12909
I893
Please store the product under the recommended conditions in the Certificate of Analysis.
Room temperature in continental US
may vary elsewhere.
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).
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].
Vanoxerine (GBR-12909) (2.5-20 mg/kg
i.p.) significantly increases the ambulatory activity[3].
Ki: 1 nM (dopamine reuptake)[1] Cellular Effect Cell Line Type Value Description References
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[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]. Andersen PH. The dopamine inhibitor GBR 12909: selectivity and molecular mechanism of action. Eur J Pharmacol. [Content Brief]
[3]. 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]