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.
|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.|
|Incubation time||24 hours - 48 hours|
|Animal models||Adult male EL mice weighing 25–30 g and adult male DDY mice|
|Administration||Administered via i.v. or p.o.|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO 25 mg/mL|
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