Nefiracetam
Based on 1 Customer Validation
Nefiracetam is a cognition-enhancing agent. Nefiracetam is an activator of nAChR, N-methyl-D-aspartate receptor (NMDAR), mGluR5, PKC, gamma-aminobutyric acid (GABA), and N/L-type Ca2+ channels. Nefiracetam promotes neuroplasticity and enhances neuroprotection. Nefiracetam can be used in Alzheimer's disease, epilepsy, and cerebral ischemia research.
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- Pureza: 99.87%
- No. CAS: 77191-36-7
- Fòrmula: C14H18N2O2
- Peso molecular:246.30
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Chemical Information
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Ver todos los productos específicos de isoformas iGluR
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Actividad biológica
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N-type calcium channel |
L-type calcium channel |
mGlu5 Receptor |
NMDA Receptor |
Nefiracetam (1-1000 nM, 10-60 min) increases rat dentate gyrus hippocampal neurotransmission (250%) in a dose-dependent manner[1].
Nefiracetam (1 μM, 20 min) enhances the activity of neuronal nAChR α3β2 (127%), α3β4 (124%), α4β2 (129%), α4β4 (112%), and α7 (178%) receptors in Xenopus oocytes[1].
Nefiracetam (1-1000 nM) improves NMDA receptor-dependent long-term potentiation (LTP) (64%) in the CA1 region of the hippocampus of OBX mice[2].
Nefiracetam (10 nM) enhances the autophosphorylation of CaMKIIα (Thr286) (77.3%) and PKCα (Ser657) (93.3%) in the CA1 region of the hippocampus of OBX mice[2].
Nefiracetam (1 μM) increases Ca2+ currents flowing through high voltage-activated (N/L-type) calcium channels in NG108-15 cells (more than 2 fold)[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Nefiracetam (10 mg/kg, i.g., once a day for 3-5 days) increases the GABA content in the right hippocampus of rats with microsphere embolization[4].
Nefiracetam (10 mg/kg, i.g., once a day for 3-5 days) increases the glutamate decarboxylase activity in the right cerebral cortex and hippocampus of rats with microsphere embolization[4].
Nefiracetam (10 mg/kg, p.o., once) inhibits Ro 5-4864 (PBR activator)-induced convulsions in EL (Epilepsy-prone Lesion) mice in a dose-dependent manner (ED50: 17.2 mg/kg) [5].
Nefiracetam (10 mg/kg, p.o., once) inhibits Ro 5-4864-induced convulsions in DDY mice (parental strain of EL mice) and spontaneous epilepsy in EL mice in a dose-dependent manner[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:OBX mice (male, 8-9 weeks old)[2]
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Dosage:0.1, 0.5, 1.0 mg/kg; 1, 10, 100, 1000 nM
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Administration:Oral gavage (p.o.)
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Result:Recovered the percentage of alteration behavior (64%).
Had no change in the total number of arms entries.
Induced enhanced levels of LTP in HFS in a dose-dependent manner.
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Animal Model:Microsphere embolization rat model (male Wistar rats, 180-220 g)[4]
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Dosage:10 mg/kg
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Administration:Intragastric administration (i.g.), once every day for 3 and 5 d
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Result:Increased GABA content in the right hippocampus.
Increased glutamate decarboxylase activity in the right cerebral cortex and hippocampus.
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Animal Model:EL mice model (adult male mice, 25-30 g)[5]
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Dosage:10 mg/kg
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Administration:Oral gavage (p.o.); Intravenous injection (i.v.), once
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Result:Inhibited Ro 5-4864-induced convulsions.
Inhibited spontaneous epilepsy in EL mice.
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Animal Model:DDY mice model (adult male mice, 30-35 g)[5]
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Dosage:10 mg/kg
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Administration:Intravenous injection (i.v.), once
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Result:Inhibited Ro 5-4864-induced convulsions in DDY mice.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 77191-36-7
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Appearance Solid
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Peso molecular 246.30
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Fòrmula C14H18N2O2
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Color White to off-white
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SMILES
O=C(NC1=C(C)C=CC=C1C)CN2C(CCC2)=O
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Synonyms
DM9384; DZL-221
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvente y solubilidad
DMSO : ≥ 100 mg/mL (406.01 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : ≥ 25 mg/mL (101.50 mM)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (10.15 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (10.15 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Pureza y Documentación
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Ficha de datos (281 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Nomura T, et al. Nefiracetam facilitates hippocampal neurotransmission by a mechanism independent of the piracetam and aniracetam action. Brain Res. 2000 Jul 7;870(1-2):157-62. [Content Brief]
[2]. Moriguchi S, et al. Nefiracetam activation of CaM kinase II and protein kinase C mediated by NMDA and metabotropic glutamate receptors in olfactory bulbectomized mice. J Neurochem. 2009 Jul;110(1):170-81. [Content Brief]
[3]. Nishizaki T, et al. A 'long-term-potentiation-like' facilitation of hippocampal synaptic transmission induced by the nootropic nefiracetam. Brain Res. 1999 May 1;826(2):281-8. [Content Brief]
[4]. Fukatsu T, et al. Effects of nefiracetam on spatial memory function and acetylcholine and GABA metabolism in microsphere-embolized rats. Eur J Pharmacol. 2002 Oct 18;453(1):59-67. [Content Brief]
[5]. Shiotani T, et al. Anticonvulsant actions of nefiracetam on epileptic EL mice and their relation to peripheral-type benzodiazepine receptors. Brain Res. 2000 Mar 24;859(2):255-61. [Content Brief]
[6]. Yoshii M, et al. Cellular mechanisms underlying cognition-enhancing actions of nefiracetam (DM-9384). Behav Brain Res. 1997 Feb;83(1-2):185-8. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 4.0601 mL | 20.3004 mL | 40.6009 mL | 101.5022 mL |
| 5 mM | 0.8120 mL | 4.0601 mL | 8.1202 mL | 20.3004 mL | |
| 10 mM | 0.4060 mL | 2.0300 mL | 4.0601 mL | 10.1502 mL | |
| 15 mM | 0.2707 mL | 1.3534 mL | 2.7067 mL | 6.7668 mL | |
| 20 mM | 0.2030 mL | 1.0150 mL | 2.0300 mL | 5.0751 mL | |
| 25 mM | 0.1624 mL | 0.8120 mL | 1.6240 mL | 4.0601 mL | |
| 30 mM | 0.1353 mL | 0.6767 mL | 1.3534 mL | 3.3834 mL | |
| 40 mM | 0.1015 mL | 0.5075 mL | 1.0150 mL | 2.5376 mL | |
| 50 mM | 0.0812 mL | 0.4060 mL | 0.8120 mL | 2.0300 mL | |
| 60 mM | 0.0677 mL | 0.3383 mL | 0.6767 mL | 1.6917 mL | |
| 80 mM | 0.0508 mL | 0.2538 mL | 0.5075 mL | 1.2688 mL | |
| 100 mM | 0.0406 mL | 0.2030 mL | 0.4060 mL | 1.0150 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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