Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 216 | 现货 | ||
50 mg | ¥ 297 | 现货 | ||
100 mg | ¥ 538 | 现货 | ||
200 mg | ¥ 796 | 现货 | ||
500 mg | ¥ 1,330 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 363 | 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 | DM9384, 奈非西坦, DZL-221 |
分子量 | 246.3 |
分子式 | C14H18N2O2 |
CAS No. | 77191-36-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 24.6 mg/mL (100 mM)
Ethanol: 24.6 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 4.0601 mL | 20.3004 mL | 40.6009 mL | 101.5022 mL |
5 mM | 0.812 mL | 4.0601 mL | 8.1202 mL | 20.3004 mL | |
10 mM | 0.406 mL | 2.03 mL | 4.0601 mL | 10.1502 mL | |
20 mM | 0.203 mL | 1.015 mL | 2.03 mL | 5.0751 mL | |
50 mM | 0.0812 mL | 0.406 mL | 0.812 mL | 2.03 mL | |
100 mM | 0.0406 mL | 0.203 mL | 0.406 mL | 1.015 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Nefiracetam 77191-36-7 Membrane transporter/Ion channel Neuroscience GABA Receptor DZL 221 γ-Aminobutyric acid Receptor DM9384 奈非西坦 DM 9384 DZL-221 inhibit Inhibitor DZL221 DM-9384 Gamma-aminobutyric acid Receptor inhibitor