产品说明书
Vanoxerine 2HCl
 |
同义名 : | GBR 12909 Dihydrochloride;I893 dihydrochloride;I 893;GBR 12909 (hydrochloride);GBR-12909;Vanoxerine dihydrochloride |
| CAS号 : | 67469-78-7 | |
| 货号 : | A268853 | |
| 分子式 : | C28H34Cl2F2N2O | |
| 纯度 : | 98% | |
| 分子量 : | 523.485 | |
| MDL号 : | MFCD00055193 | |
| 存储条件： |
粉末 Sealed in dry,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 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 |
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| 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]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.91mL 0.38mL 0.19mL |
9.55mL 1.91mL 0.96mL |
19.10mL 3.82mL 1.91mL |
| 参考文献 |
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