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 (Ki=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]。
参考详情:Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) | Dopamine Transporter抑制剂 | MCE
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.