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Membrane transporter/Ion channel GABA Receptor Nefiracetam

Nefiracetam

Catalog No. T0169   CAS 77191-36-7
Synonyms: DZL-221, DM9384

Nefiracetam are underway in Phase 2 trials. Nefiracetam, a GABAergic、 cholinergic、and monoaminergic neuronal system enhancer, is used for Ro 5-4864-induced convulsions.

Nefiracetam, CAS 77191-36-7
Pack Size Availability Price/USD Quantity
25 mg In stock 38.00
50 mg In stock 50.00
100 mg In stock 65.00
250 mg In stock 97.00
1 mL * 10 mM (in DMSO) In stock 50.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Nefiracetam are underway in Phase 2 trials. Nefiracetam, a GABAergic、 cholinergic、and monoaminergic neuronal system enhancer, is used for Ro 5-4864-induced convulsions.
Targets&IC50 GABAR,  
Kinase Assay Assay of glutamate released: 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 Research
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. (Only for Reference)
Cell lines: Oocytes
Synonyms DZL-221 , DM9384
Purity 90.88%
Molecular Weight 246.31
Formula C14H18N2O2
CAS No. 77191-36-7

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 24.6 mg/mL (100 mM)

Ethanol: 24.6 mg/mL (100 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Shiotani T, et al. Brain Res, 2000, 859(2), 255-261. 2. Yoshii M, et al. Brain Res, 1994, 642(1-2), 123-131. 3. Nishizaki T, et al. Mol Pharmacol, 1998, 53(1), 1-5. 4. Nishizaki T, et al. Brain Res Mol Brain Res, 2000, 80(1), 53-62. 5. Sakurai T, et al. Jpn J Pharmacol, 1989, 50(1), 47-53.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Clinical Compound Library Neuronal Signaling Compound Library Ion Channel Inhibitor Library GPCR Compound Library

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