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伐诺司林二盐酸盐 /Vanoxerine 2HCl {[allProObj[0].p_purity_real_show]}

货号:A268853 同义名: GBR 12909 Dihydrochloride;I893 dihydrochloride

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

Vanoxerine 2HCl 化学结构 CAS号:67469-78-7
Vanoxerine 2HCl 化学结构
CAS号:67469-78-7
Vanoxerine 2HCl 3D分子结构
CAS号:67469-78-7
Vanoxerine 2HCl 化学结构 CAS号:67469-78-7
Vanoxerine 2HCl 3D分子结构 CAS号:67469-78-7
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Vanoxerine 2HCl 纯度/质量文件 产品仅供科研

货号:A268853 标准纯度: {[allProObj[0].p_purity_real_show]}
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Vanoxerine 2HCl 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].

Vanoxerine 2HCl 参考文献

[1]Melia KF, Spealman RD. Pharmacological characterization of the discriminative-stimulus effects of GBR 12909. J Pharmacol Exp Ther. 1991 Aug;258(2):626-32.

[2]Heikkila RE, Manzino L. Behavioral properties of GBR 12909, GBR 13069 and GBR 13098: specific inhibitors of dopamine uptake. Eur J Pharmacol. 1984 Aug 17;103(3-4):241-8.

[3]Rothman RB, Baumann MH, Prisinzano TE, Newman AH. Dopamine transport inhibitors based on GBR12909 and benztropine as potential medications to treat cocaine addiction. Biochem Pharmacol. 2008;75(1):2-16

[4]Hirate K, Kuribara H. Characteristics of the ambulation-increasing effect of GBR-12909, a selective dopamine uptake inhibitor, in mice. Jpn J Pharmacol. 1991;55(4):501-511

[5]Andersen PH. The dopamine inhibitor GBR 12909: selectivity and molecular mechanism of action. Eur J Pharmacol. 1989;166(3):493-504

Vanoxerine 2HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.91mL

0.38mL

0.19mL

9.55mL

1.91mL

0.96mL

19.10mL

3.82mL

1.91mL

Vanoxerine 2HCl 技术信息

CAS号67469-78-7
分子式C28H34Cl2F2N2O
分子量 523.485
别名 GBR 12909 Dihydrochloride;I893 dihydrochloride;I 893;GBR 12909 (hydrochloride);GBR-12909;Vanoxerine dihydrochloride
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Room Temperature

溶解度

DMSO: 8 mg/mL(15.28 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 1 mg/mL(1.91 mM),配合低频超声,并水浴加热至45℃助溶

动物实验配方
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