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Nefiracetam (DM9384) 是一种 GABA 能、胆碱能和单胺能神经元系统增强剂,用于治疗 Ro 5-4864 引起的抽搐。
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Nefiracetam (DM9384) 是一种 GABA 能、胆碱能和单胺能神经元系统增强剂,用于治疗 Ro 5-4864 引起的抽搐。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
25 mg | ¥ 123 | 现货 | |
50 mg | ¥ 163 | 现货 | |
100 mg | ¥ 263 | 现货 | |
500 mg | ¥ 662 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 218 | 现货 |
产品描述 | Nefiracetam (DM9384) are underway in Phase 2 trials. Nefiracetam, a GABAergic、 cholinergic、and monoaminergic neuronal system enhancer, is used for Ro 5-4864-induced convulsions. |
体外活性 | 在DDY小鼠体内,Nefiracetam(>10 mg/kg)也会有效抑制Ro 5-4864诱导的抽搐.口服Nefiracetam可抑制EL小鼠体内Ro 5-4864诱导的惊厥.在每次训练项目前,Nefiracetam给药(1 time/day)有利于回避反应的获得过程. |
体内活性 | Nefiracetam(0.01–0.1 μM)诱导Ach激发电流的短期抑制,Nefiracetam(1–10 μM)对电流具有长期增强作用。1 μM的Nefiracetam增加2倍钙通道电流的长效组分,而不改变瞬变组分。Nefiracetam处理10分钟后,Ach诱发的电流减少到对照组的30% (0.01 μM)和38%(0.1 μM)。Nefiracetam可与PKC通路发生相互作用提高烟碱Ach受体的活性,进而增加从突出前末梢谷氨酸的释放量,使海马神经传递的持久易化。认知能力增强剂发挥作用的细胞机理可能是通过Nefiracetam与PKA和PKC通路的相互作用造成的。在大鼠海马神经元的原代培养中,Nefiracetam增加烟碱敏感的兴奋性突触后电流比率。在大鼠海马切片的CA1区和齿状回中,Nefiracetam诱导突触传导的持久易化, α-银环蛇毒素和美加明可抑制该易化作用。 |
激酶实验 | Assay of glutamate released: Hippocampal slices (400 μM) are prepared from the guinea pig brain using standard techniques. A slice is fixed on a pair of silver wire electrodes (10 Hz, 5 V, 0.1 ms in duration) at 1-minutes intervals for 10 minutes and submerged in 1 mL standard artificial cerebrospinal fluid (ACSF) (in mM: 125 mM NaCl, 5 mM KCl, 1.24 mM KH2PO4, 1.3 mM MgSO4, 2 mM CaCl2, 26 mM NaHCO3, and 10 mM glucose) oxygenated with 95% O2 and 5% CO2 at 36 °C in the presence and absence of tetrodotoxin (TTX) (0.5 μM). In a different set of experiments, electrical stimulation is applied to slices treated with Nefiracetam (1 μM) in the presence and absence of α-bungarotoxin (50 nM) or mecamylamine (3 μM). A 100 μL aliquot of the medium filtered with millipore filters (0.45 μM) is injected onto the cation-exchanger column of the autoanalyser to separate amino acids and the amount of glutamate released is calculated using known amino acid standard concentrations. |
细胞实验 | The injected oocytes are transferred to the recording chamber 24 to 48 hours after incubation and continuously superfused at room temperature (20 to 22 °C) in a standard frog Ringer's solution (115 mM NaCl, 2 mM KCl, 1.8 mM CaCl2, and 5 mM HEPES, pH 7.0). Ca2+ -free extracellular solution consisted of 115 mM NaCl, 2 mM KCl, 5 mM MgCl2, 5 mM HEPES, and 1 mM EGTA, pH 7.0. To remove the effect of the muscarinic ACh receptor, 1 μM atropine is added to the extracellular solution. ACh-activated currents are recorded using two-electrode, voltage-clamp techniques. The currents are analyzed on a microcomputer using pClamp software. ACh is bath-applied to oocytes. Nefiracetam is dissolved in distilled water at 1 mM for stock solution and diluted into concentrations required with the extracellular solution. (Only for Reference) |
别名 | 奈非西坦, DM9384, DZL-221 |
分子量 | 246.3 |
分子式 | C14H18N2O2 |
CAS No. | 77191-36-7 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 70 mg/mL (284.21 mM), Sonication is recommended. Ethanol: 24.6 mg/mL (100 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
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