Nefiracetam

ArtNr	S1969-5000
Hersteller	Selleckchem
CAS-Nr.	77191-36-7
Menge	5 g
Quantity options	1 g 10 g 10 mM/1 ml 250 mg 50 mg 5 g
Kategorie	Neuroscience Molecular Targets for Neuroscience Inhibitors & Compound Libraries Small Molecules
Typ	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
Lieferbar
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 25â€“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 (0.01â€“0.1 uM) and a long-term enhancement of the currents at micromolar concentrations (1â€“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.

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