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    Nefiracetam (DM9384; DZL-221)
    Nefiracetam (DM9384; DZL-221)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1288
    CAS #: 77191-36-7Purity ≥98%

    Description: Nefiracetam (DZL-221; DM9384; DZL221; DM 9384; Translon) is a potent GABAergic, cholinergic, and monoaminergic neuronal system enhancer for Ro 5-4864-induced convulsions. It is a nootropic (cognition-enhancing) agent with antidementia activity. Nefiracetam at a concentration of 1 μM increases a long-lasting component of calcium channel currents two-fold without affecting a transient component. Nefiracetam induces a short-term depression of ACh-evoked currents at submicromolar concentrations (0.01–0.1 μM) and a long-term enhancement of the currents at micromolar concentrations (1–10 μM). 

    References: Brain Res. 2000 Mar 24;859(2):255-61; Brain Res. 1994 Apr 11;642(1-2):123-31.

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    Molecular Weight (MW)246.3
    FormulaC14H18N2O2 
    CAS No.77191-36-7
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 49 mg/mL (198.9 mM)
    Water: 5 mg/mL (20.3 mM)
    Ethanol: 49 mg/mL (198.9 mM)
    Solubility (In vivo)

    Chemical Name: N-(2,6-dimethylphenyl)-2-(2-oxopyrrolidin-1-yl)acetamide

    InChi Key: NGHTXZCKLWZPGK-UHFFFAOYSA-N

    InChi Code: InChI=1S/C14H18N2O2/c1-10-5-3-6-11(2)14(10)15-12(17)9-16-8-4-7-13(16)18/h3,5-6H,4,7-9H2,1-2H3,(H,15,17)

    SMILES Code: O=C(NC1=C(C)C=CC=C1C)CN2C(CCC2)=O

    SynonymsDZL 221; DM-9384; DZL-221; DM9384; DZL221; DM 9384; Translon


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    In Vitro

    In vitro activity: Nefiracetam at a concentration of 1 μM increases a long-lasting component of calcium channel currents two-fold without affecting a transient component. Nefiracetam induces a short-term depression of ACh-evoked currents at submicromolar concentrations (0.01–0.1 μM) and a long-term enhancement of the currents at micromolar concentrations (1–10 μM). Nefiracetam interacts with PKA and PKC pathways, which may explain a cellular mechanism for the action of cognition-enhancing agents. Lower (submicromolar) concentrations of the nootropic Nefiracetam reduces ACh-evoked currents to 30% (0.01 μM) and 38% (0.1 μM) of control after a 10-minute treatment. In primary cultures of rat hippocampal neurons, nefiracetam increases the rate of nicotine-sensitive miniature excitatory postsynaptic currents. Nefiracetam induces a long-lasting facilitation of synaptic transmission in both the CA1 area and the dentate gyrus of rat hippocampal slices, and the facilitation is inhibited by α-bungarotoxin and mecamylamine. Nefiracetam enhances activity of nicotinic ACh receptors by interacting with a PKC pathway, thereby increasing glutamate release from presynaptic terminals, and then leading to a sustained facilitation of hippocampal neurotransmission. 


    Kinase Assay:  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.


    Cell Assay:  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.

    In VivoNefiracetam administered orally inhibits Ro 5-4864-induced convulsions in EL mice. Nefiracetam also efficiently inhibits Ro 5-4864-induced convulsions in DDY mice at doses higher than 10 mg/kg. Nefiracetam administered daily 1 hour before each training session facilitates the acquisition process of the avoidance response. 
    Animal modelMice
    Formulation & DosageOral
    References

    Brain Res. 2000 Mar 24;859(2):255-61; Brain Res. 1994 Apr 11;642(1-2):123-31.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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