CAS:67469-78-7Vanoxerine Dihydrochloride

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Synonyms: GBR-12909 2HCl;I-893 2HCl

Vanoxerine 2HCl is a selcetive and potent Dopamine reuptake inhibitor (DRI).

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18817579266

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18817579266

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实验数据

技术信息

CAS号

67469-78-7

储存条件

分子式

C28H34Cl2F2N2O

运输

蓝冰

分子量

523.49

别名

GBR-12909 2HCl;I-893 2HCl

溶解度

DMSO	17.0 mg/mL (32.5 mM)
Ethanol	2.0 mg/mL (3.8 mM)

动物实验配方

生物活性

描述Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) is a competitive, potent, and highly selective dopamine reuptake inhibitor (Ki = 1 nM). Vanoxerine dihydrochloride binds to the target site on the dopamine transporter (DAT)^[3]. Vanoxerine 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. The neurochemical experiment in rats, not in mice, revealed that vanoxerine possessed more dominant action on dopaminergic systems than noradrenergic or serotonergic systems^[4]. Vanoxerine dihydrochloride is also an oral, mixed ion channel blocker with IKr, INa, and L-type calcium channel activity. Vanoxerine inhibits dopamine uptake by binding to the dopamine binding site on the carrier protein itself, thereby blocking the carrier process^[5].