Nefiracetam (Translon) 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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 40 mg/mL|
|Related GABA Receptor Products|
ONO-8590580 is a GABAAα5 negative allosteric modulator which enhances long-term potentiation and improves cognitive deficits in preclinical models.
LAU159 is a potent, functionally selective α6β3γ2 GABAA receptor modulator.
Aminooxyacetic acid hemihydrochloride is a malate-aspartate shuttle (MAS) inhibitor which also inhibits the GABA degradating enzyme GABA-T.
Chlormethiazole hydrochloride is a GABAA agonist; glycine receptor modulator.
Tiagabine Hydrochloride is the hydrochloride salt form of tiagabine, a nipecotic acid derivative with anticonvulsant property. A selective gamma-aminobutyric acid (GABA) reuptake inhibitor.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.