Vanoxerine (dihydrochloride)

MCE 国际站：Vanoxerine (dihydrochloride)

CAS：67469-78-7

品牌：MedChemExpress (MCE)

存储条件：4°C, sealed storage, away from moisture

生物活性：Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) 是一种竞争性、有效且高度选择性的多巴胺再摄取抑制剂 (K_i=1 nM)。 Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) 与多巴胺转运体 (DAT) 上的靶位点结合^[1]。 IC50 和目标：Ki：1 nM（多巴胺再摄取）^[1]  

体外：Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) 抑制多巴胺 (DA) 的摄取，IC₅₀ 在低纳摩尔范围内，作为去甲肾上腺素和 5 -HT^[2].Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) 也是一种口服的混合离子通道阻滞剂，具有 IKr、INa 和 L 型钙通道活性^{[ 3]}。

体内：Vanoxerine dihydrochloride（2.5-20 mg/kg；腹腔注射）显着增加行走活动^[3]。

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研究领域：Neuronal Signaling

作用靶点：Dopamine Transporter

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参考文献：[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.