Comparison

Nefiracetam European Partner

Item no. S1969-1000
Manufacturer Selleckchem
CASRN 77191-36-7
Amount 1 g
Quantity options 1 g 10 g 10 mM/1 ml 250 mg 50 mg 5 g
Category
Type Inhibitors
Specific against other
Smiles CC1=C(C(=CC=C1)C)NC(=O)CN2CCCC2=O
ECLASS 10.1 32160490
ECLASS 11.0 32160490
UNSPSC 12000000
Alias DZL 221
Similar products Nefiracetam
Available
Storage Conditions
2 years -80 in solvent
Molecular Weight
246, 3
Administration
Administered via i.v. or p.o.
Animal Models
Adult male EL mice weighing 25–30 g and adult male DDY mice
Cell lines
Oocytes
Concentrations
ca.1 uM
Dosages
10 mg/kg
In vitro
Nefiracetam at a concentration of 1 uM increases a long-lasting component of calcium channel currents two-fold without affecting a transient component. [2] Nefiracetam induces a short-term depression of ACh-evoked currents at submicromolar concentrations (0.01–0.1 uM) and a long-term enhancement of the currents at micromolar concentrations (1–10 uM). 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 uM) and 38% (0.1 uM) of control after a 10-minute treatment [3] 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 alpha-bungarotoxin and mecamylamine.iracetam 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. [4]
In vivo
Nefiracetam 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. [1] Nefiracetam administered daily 1 hour before each training session facilitates the acquisition process of the avoidance response. [5]
Incubation Time
24 hours - 48 hours
Kinase Assay
[4], Assay of glutamate released, Hippocampal slices (400 uM) 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 uM). In a different set of experiments, electrical stimulation is applied to slices treated with Nefiracetam (1 uM) in the presence and absence of alpha-bungarotoxin (50 nM) or mecamylamine (3 uM). A 100 uL aliquot of the medium filtered with millipore filters (0.45 uM) 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.
Method
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 uM 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.
Solubility (25C)
DMSO 49 mg/mL, Water 5 mg/mL, Ethanol 49 mg/mL
Information
Nefiracetam (DZL 221) is a GABAergic, cholinergic, and monoaminergic neuronal system enhancer for Ro 5-4864-induced convulsions. Phase 2.

Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.

All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.

Amount: 1 g
Available: In stock
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