Tetrabenazine (Ro 1-9569) 是一种可逆的囊泡单胺转运蛋白VMAT2位点抑制剂,其Kd值为 1.34 nM,可用于亨廷顿舞蹈病等多动性运动障碍相关疾病研究。
生物活性 | Tetrabenazine (Ro 1-9569) is a reversible inhibitor of the vesicularmonoamine transporterVMAT2with theKdvalue of 1.34 nM. Tetrabenazine can be used for research on diseases related to hyperactive movement disorders such as Huntington's disease[1][2][3]. |
体内研究 (In Vivo) | Tetrabenazine (subcutaneous injection, 1-10 mg/kg, once) can reduce the aggressive behavior in a dose-dependent manner and the levels of neurotransmitter molecules NE, DA and 5-HT in adult male mice[1].Tetrabenazine (intraperitoneal injection, 0-2 mg/kg, once) has selective effects on movement which can significantly attenuate morphine-induced hypermobility but oral tremors and stereotyped behaviors in male ICR mice[2].Tetrabenazine (intraperitoneal injection, 0.25-2 mg/kg, once a week) increases tremulous jaw movement (TJM) in a dose-dependent manner in adult male Sprague-Dawley rat[3].
Animal Model: | Adult male MAO A KO or wide type mice aged 1-2 months[1] | Dosage: | 1-10 mg/kg | Administration: | Subcutaneous injection; once | Result: | Completely eliminated the aggressive behavior at a concentration of 5 mg/kg and significantly reduced their NE, DA and 5-HT levels. |
Animal Model: | Male ICR mice (10 weeks old)[2] | Dosage: | 0-2 mg/kg | Administration: | Intraperitoneal injection; once | Result: | Attenuated the subsequent morphine-induced hypermobility after pretreatment with tetrabenazine. Reduced METH-induced increases in locomotion at 1 mg/kg. |
Animal Model: | Adult male Sprague-Dawley rat weighed 350-450 g[3] | Dosage: | 0.25-2 mg/kg | Administration: | Intraperitoneal injection; once a week | Result: | Induced tremulous jaw movement (TJM) significantly at the concentration of 2 mg/kg and more motor impairments with higher doses such as 3-4 mg/kg. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 33.33 mg/mL(105.00 mM;Need ultrasonic) H2O :< 0.1 mg/mL (ultrasonic)(insoluble) 配制储备液 1 mM | 3.1504 mL | 15.7520 mL | 31.5040 mL | 5 mM | 0.6301 mL | 3.1504 mL | 6.3008 mL | 10 mM | 0.3150 mL | 1.5752 mL | 3.1504 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (7.88 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.88 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (7.88 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.88 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (7.88 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.88 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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