Aniracetam (Ro 13-5057) 是一种具有口服活性神经保护剂，具有益智活性。Aniracetam 增强了大鼠海马体切片CA1区离子转变 quisqualate (iQA) 反应。Aniracetam 还增强了 Schaffer 旁系联合突触的兴奋性突触后电位 (EPSPs)。Aniracetam 可预防高碳酸血症模型大鼠 CO2所致的习得障碍。Aniracetam 可用于研究脑功能障碍。
| 生物活性 | Aniracetam (Ro 13-5057) is an orally active neuroprotective agent, possessing nootropics effects. Aniracetam potentiates the ionotropic quisqualate (iQA) responses in the CA1 region of rat hippocampal slices. Aniracetam also potentiates the excitatory post synaptic potentials (EPSPs) in Schaffer collateral-commissural synapses. Aniracetam can prevents the CO2-induced impairment of acquisition in hypercapnia model rats. Aniracetam can be used to research cerebral dysfunctional disorders[1][2][3][4]. |
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体外研究
(In Vitro) | Aniracetam concentration-dependently counteracts glutsmate-, kainate-, or α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid-induced cell death and greatly facilitated neuroprotective response achieved by different concentrations of both quisqualate and trans-1-aminocyclopentane-1, 3-dicarboxylate in primary cultures of cerebellar granule cells[4].
Aniracetam potentiates the mGluR-coupled stimulation of phospholipase C in primary cultures of cerebellar granule cells[4].
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体内研究
(In Vivo) | Aniracetam (1 mM; 30-75 min) potentiates the iQA receptors and produces remarkable facilitation of the native synaptic transmission in rats[1].
Aniracetam (10-100 mg/kg; p.o.; single dosage) prevents the CO2-induced impairment of acquisition in rats[2].
Aniracetam (30-300 mg/kg; p.o.; single dosage) increases the percentage of rats showing passive avoidance[2].
| Animal Model: | Pyramidal neurons from male Wistar rats[1] | | Dosage: | 1 mM | | Administration: | 30-75 min | | Result: | Potentiated the iQA receptors existing in the brain and produced remarkable facilitation of the native synaptic transmission. |
| Animal Model: | Male rats (100-120 g; hypercapnia induced by pure CO2)[2] | | Dosage: | 10, 30, 50 and 100 mg/kg | | Administration: | p.o.; single dosage (60 min before hypercapnia) | | Result: | Significantly prevented the CO2-induced impairment of acquisition at 30 and 50 mg/kg. |
| Animal Model: | Male rats and male mice (100-120 g and 21-25 g; 0.5 mg/kgScopolamine-induced transient disruption of the memory of a passive avoidance procedure)[2] | | Dosage: | 30, 50, 100 and 300 mg/kg, | | Administration: | p.o.; single dosage | | Result: | Significantly increased the percentage of rats showing passive avoidance 2 h afterScopolamine(HY-N0296) at 50 and 100 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 : ≥ 100 mg/mL(456.12 mM) H2O : 0.33 mg/mL(1.51 mM;Need ultrasonic) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 4.5612 mL | 22.8061 mL | 45.6121 mL | | 5 mM | 0.9122 mL | 4.5612 mL | 9.1224 mL | | 10 mM | 0.4561 mL | 2.2806 mL | 4.5612 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 (11.40 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (11.40 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 (11.40 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (11.40 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 (11.40 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (11.40 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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