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Nefiracetam is cognitive enhancer with an IC50 of approximately 150–200 μM for Ro 5-4864. It displays various pharmacological effects. It activates L/N-type calcium channels, cholinergic, monoaminergic and GABAergic systems. It displays potent neuroprotective action in the retinal ischemia-reperfusion model in vivo.
| Cell Experiment | |
|---|---|
| Cell lines | Oocytes |
| Preparation method | Transferring the injected oocytes 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, adding 1 μM atropine the extracellular solution. Using two-electrode, voltage-clamp techniques to record ACh-activated currents. Analyzing the currents 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 which are required with the extracellular solution. |
| Concentrations | ~1 μM |
| Incubation time | 24 hours - 48 hours |
| Animal Experiment | |
|---|---|
| Animal models | Adult male EL mice weighing 25–30 g and adult male DDY mice |
| Formulation | |
| Dosages | |
| Administration | Administered via i.v. or p.o. |
| Molecular Weight | 246.3 |
| Formula | C14H18N2O2 |
| CAS Number | 77191-36-7 |
| Solubility (25°C) | DMSO 25 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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