| 中文名称 |
Nefiracetam
|
| 中文别名 |
奈非西坦;N-(2,6-二甲基苯基)-2-氧代-1-吡咯烷乙酰胺;N-(2,6-二甲苯基)-2-氯乙酰胺;Nefiracetam 奈非西坦;N-(2,6-二甲苯基)-2-(2-氧吡咯烷-1-基)乙酰胺
|
| 英文名称 |
Nefiracetam
|
| 英文别名 |
N-(2,6-Dimethylphenyl)-2-(2-oxopyrrolidin-1-yl)acetamide;n-(2,6-dimethylphenyl)-2-oxo-1-pyrrolidineacetamide;[(2,6-dimethylphenyl)aminocarbonylmethyl]chloride;Nefiracetam;1-Pyrrolidineacetamide,N-(2,6-dimethylphenyl)-2-oxo-;DM9384;DZL221;DZL-221;(2-(2-oxopyrrolidin-1-yl)-N-(2,6-dimethylphenyl)-acetamide);DM-9384;N-(2,6-Dimethylphenyl)-2-oxo-1-pyrrolidineacetamide
|
| Cas No. |
77191-36-7
|
| 分子式 |
C14H18N2O2
|
| 分子量 |
246.30
|
| 包装储存 |
Powder -20°C 3 years;4°C 2 years
|
| 详情描述 |
Nefiracetam作用于Ro 5-4864引起的抽搐,是GABAergic,胆碱及单胺类的神经系统增强剂。
|
| 产品详情 |
Nefiracetam作用于Ro 5-4864引起的抽搐,是GABAergic,胆碱及单胺类的神经系统增强剂。
|
| 生物活性 |
Nefiracetam is a GABAergic, cholinergic, and monoaminergic neuronal systems enhancer for Ro 5-4864-induced convulsions.
Target: GABA Receptor
Nefiracetam induces a short-term depression of ACh-evoked currents at submicromolar concentrations (0.01-0.1 μM) and a long-term enhancement of the currents at micromolar concentrations (1-10 μM). Nefiracetam interacts with PKA and PKC pathways, which may explain a cellular mechanism for the action of cognition-enhancing agents. Lower (submicromolar) concentrations of the nootropic Nefiracetam reduces ACh-evoked currents to 30% (0.01 μM) and 38% (0.1 μM) of control after a 10-minute treatment [1].
Nefiracetam administered orally inhibits Ro 5-4864-induced convulsions in EL mice. Nefiracetam also efficiently inhibits Ro 5-4864-induced convulsions in DDY mice at doses higher than 10 mg/kg [2]. Nefiracetam administered daily 1 hour befo
|
| 性状 |
Solid
|
| 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
|
| ClinicalTrial |
|
| 参考文献 |
[1]. Nishizaki, T., et al., Nefiracetam modulates acetylcholine receptor currents via two different signal transduction pathways. Mol Pharmacol, 1998. 53(1): p. 1-5.[2]. Shiotani, T., et al., Anticonvulsant actions of nefiracetam on epileptic EL mice and their relation to peripheral-type benzodiazepine receptors. Brain Res, 2000. 859(2): p. 255-61.
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| 溶解度数据 |
In Vitro: DMSO : ≥ 100 mg/mL (406.01 mM)H2O : ≥ 25 mg/mL (101.50 mM)
|
[1]. Nishizaki, T., et al., Nefiracetam modulates acetylcholine receptor currents via two different signal transduction pathways. Mol Pharmacol, 1998. 53(1): p. 1-5.[2]. Shiotani, T., et al., Anticonvulsant actions of nefiracetam on epileptic EL mice and their relation to peripheral-type benzodiazepine receptors. Brain Res, 2000. 859(2): p. 255-61.
1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。
2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。