Flumazenil

製品コードS1332 バッチS133205

印刷

化学情報

Synonyms

RO 15-1788

Storage
(From the date of receipt)

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

化学式

C₁₅H₁₄FN₃O₃

分子量

303.29

CAS No.

78755-81-4

Solubility (25°C)*

体外

DMSO

31 mg/mL (102.21 mM)

Ethanol

5 mg/mL (16.48 mM)

Water

Insoluble

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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	1.550mg/ml (5.11mM)	Taking the 1 mL working solution as an example, add 50 μL of 31 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	1.550mg/ml (5.11mM)	Taking the 1 mL working solution as an example, add 50 μL of 31 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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	Flumazenil is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.
in vivo	Flumazenil interacts at the central benzodiazepine receptor to antagonize or reverse the behavioral, neurologic, and electrophysiologic effects of benzodiazepine agonists and inverse agonists. This compound is of some benefit in hepatic encephalopathy, but until well-designed clinical trials are conducted, hepatic encephalopathy must be considered an investigational indication for flumazenil. It has been shown to reverse sedation caused by intoxication with benzodiazepines alone or benzodiazepines in combination with other agents, but it should not be used when cyclic antidepressant intoxication is suspected. ^[1] This chemical (1 mg/kg) induces a strong anxiolytic effect in BALB/c mice tested in the elevated plus maze and light/dark test. ^[2] It (10 mg/kg) effectively prevents the reduction produced by allopregnanolone in rats. ^[3] This compound (5-20 mg/kg) antagonizes the anticonvulsant and adverse effects of diazepam but not GYKI 52466 in mice. It slightly reduces the anticonvulsant activity of NBQX in the MES model but not in the PTZ test. ^[4] This chemical (3.0 mg/kg) blocks the changes withdrawal from chronic ethanol treatment, which leads to a decrease in open arm time and percent open arm entries. ^[5]

製品説明

Flumazenil is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.

in vivo

Flumazenil interacts at the central benzodiazepine receptor to antagonize or reverse the behavioral, neurologic, and electrophysiologic effects of benzodiazepine agonists and inverse agonists. This compound is of some benefit in hepatic encephalopathy, but until well-designed clinical trials are conducted, hepatic encephalopathy must be considered an investigational indication for flumazenil. It has been shown to reverse sedation caused by intoxication with benzodiazepines alone or benzodiazepines in combination with other agents, but it should not be used when cyclic antidepressant intoxication is suspected. ^[1] This chemical (1 mg/kg) induces a strong anxiolytic effect in BALB/c mice tested in the elevated plus maze and light/dark test. ^[2] It (10 mg/kg) effectively prevents the reduction produced by allopregnanolone in rats. ^[3] This compound (5-20 mg/kg) antagonizes the anticonvulsant and adverse effects of diazepam but not GYKI 52466 in mice. It slightly reduces the anticonvulsant activity of NBQX in the MES model but not in the PTZ test. ^[4] This chemical (3.0 mg/kg) blocks the changes withdrawal from chronic ethanol treatment, which leads to a decrease in open arm time and percent open arm entries. ^[5]

プロトコル(参考用のみ)

参考

https://pubmed.ncbi.nlm.nih.gov/8306565/
https://pubmed.ncbi.nlm.nih.gov/10663414/
https://pubmed.ncbi.nlm.nih.gov/8566110/

https://pubmed.ncbi.nlm.nih.gov/7889291/
https://pubmed.ncbi.nlm.nih.gov/9226737/

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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Inhibition of GABAA receptors in intestinal stem cells prevents chemoradiotherapy-induced intestinal toxicity [ J Exp Med, 2022, 219-12e20220541]	PubMed: 36125780
Evaluation of the role of different neurotransmission systems in the anticonvulsant action of sildenafil in the 6 Hz-induced psychomotor seizure threshold test in mice [Nieoczym D Biomed Pharmacother, 2018, 107:1674-1681]	PubMed: 30257385
Investigation of the Anxiolytic and Antidepressant Effects of Curcumin, a Compound From Turmeric (Curcuma longa), in the Adult Male Sprague-Dawley Rat [Ceremuga TE Holist Nurs Pract, 2017, 31(3):193-203]	PubMed: 28406873

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。