Nefiracetam

SKU: orb1310875

Description

Nefiracetam (DM9384), a modulator of GABAergic, cholinergic, and monoaminergic systems, is under Phase 2 clinical investigation. It has demonstrated efficacy in preclinical models, such as suppressing Ro 5-4864-induced convulsions in vivo, supporting research in neuroscience and cognitive disorders.

Research Area

Epigenetics & Chromatin, Metabolism Research, Neuroscience, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 77191-36-7
• MW: 246.3
• Purity: >99.99% (May vary between batches)
• Formula: C₁₄H₁₈N₂O₂
• SMILES: N(C(CN1C(=O)CCC1)=O)C2=C(C)C=CC=C2C
• Target: Calcium Channel,GluR,iGluR,GABA Receptor,PKC,AChR
• Solubility: DMSO:70 mg/mL (284.21 mM);Ethanol:24.6 mg/mL (99.88 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (8.12 mM)

Bioactivity

• In Vivo:
  Nefiracetam, at low concentrations (0.01–0.1 μM), induces a transient inhibition of Ach-evoked currents, while at higher concentrations (1–10 μM), it provides a sustained enhancement of these currents. Specifically, 1 μM Nefiracetam doubles the long-lasting component of the calcium channel current without affecting the transient component. After a 10-minute treatment with Nefiracetam, Ach-induced current is reduced to 30% at 0.01 μM and 38% at 0.1 μM of the control levels. The compound interacts with the PKC pathway, augmenting the activity of nicotinic Ach receptors, thereby increasing the release of presynaptic glutamate, and leading to potentiation of synaptic transmission in the hippocampus. This mechanism may underlie cognitive enhancement elicited by Nefiracetam through its interaction with PKA and PKC pathways. In primary cultures of rat hippocampal neurons, Nefiracetam increases the ratio of nicotinic-sensitive excitatory postsynaptic currents. Moreover, in rat hippocampal slices in both the CA1 region and the dentate gyrus, Nefiracetam induces long-lasting synaptic potentiation, which can be inhibited by α-bungarotoxin and mecamylamine.
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• In Vitro:
  In DDY mice, Nefiracetam (>10 mg/kg) effectively inhibits convulsions induced by Ro 5-4864. Oral administration of Nefiracetam suppresses Ro 5-4864-induced seizures in EL mice. Administering Nefiracetam (1 time/day) prior to each training session facilitates the acquisition of avoidance responses.
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• 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)
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

DZL 221, DZL221, DZL-221, DM 9384, DM9384, DM-9384, GABAReceptor, Gamma-aminobutyric acid Receptor, GABAR, GABA Receptor, Inhibitor, Nefiracetam, inhibit, γ-Aminobutyric acid Receptor

Compound Identifiers

PubChem CID

71157