Nefiracetam

製品コードS1969 バッチS196901

印刷

化学情報

Synonyms

DZL 221

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₄H₁₈N₂O₂

分子量

246.3

CAS No.

77191-36-7

Solubility (25°C)*

体外

DMSO

49 mg/mL (198.94 mM)

Ethanol

49 mg/mL (198.94 mM)

Water

3 mg/mL (12.18 mM)

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Nefiracetam (DZL 221) は、Ro 5-4864誘発痙攣に対するGABAergic、cholinergic、およびmonoaminergicニューロンシステムエンハンサーです。フェーズ2。
in vitro	Nefiracetam at a concentration of 1 μM increases a long-lasting component of calcium channel currents two-fold without affecting a transient component. This compound induces a short-term depression of ACh-evoked currents at submicromolar concentrations (0.01–0.1 μM) and a long-term enhancement of the currents at micromolar concentrations (1–10 μM). It 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 reduces ACh-evoked currents to 30% (0.01 μM) and 38% (0.1 μM) of control after a 10-minute treatment. In primary cultures of rat hippocampal neurons, this compound increases the rate of nicotine-sensitive miniature excitatory postsynaptic currents. It 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 α-bungarotoxin and mecamylamine. This chemical 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.
in vivo	Nefiracetam administered orally inhibits Ro 5-4864-induced convulsions in EL mice. This compound also efficiently inhibits Ro 5-4864-induced convulsions in DDY mice at doses higher than 10 mg/kg. It administered daily 1 hour before each training session facilitates the acquisition process of the avoidance response.

プロトコル(参考用のみ)

キナーゼアッセイ	Assay of glutamate released
キナーゼアッセイ	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 this compound (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.
細胞アッセイ	細胞株	Oocytes
	濃度	~1 μM
	反応時間	24 hours - 48 hours
	実験の流れ	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. This compound is dissolved in distilled water at 1 mM for stock solution and diluted into concentrations required with the extracellular solution.
動物実験	動物モデル	Adult male EL mice weighing 25–30 g and adult male DDY mice
	投薬量	10 mg/kg
	投与方法	Administered via i.v. or p.o.

参考

https://pubmed.ncbi.nlm.nih.gov/10719072/
https://pubmed.ncbi.nlm.nih.gov/8032872/
https://pubmed.ncbi.nlm.nih.gov/9443926/

https://pubmed.ncbi.nlm.nih.gov/11039729/
https://pubmed.ncbi.nlm.nih.gov/2724699/

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長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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