Vanoxerine_product_DataBase

Bioactivity	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].
Target	Ki: 1 nM (dopamine reuptake)
Invitro	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].
In Vivo	Vanoxerine (GBR-12909) (2.5-20 mg/kg; i.p.) significantly increases the ambulatory activity[3]. Animal Model:
Name	Vanoxerine
CAS	67469-69-6
Formula	C28H32F2N2O
Molar Mass	450.56
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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. [2]. Andersen PH. The dopamine inhibitor GBR 12909: selectivity and molecular mechanism of action. Eur J Pharmacol. [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.

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