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Flumazenil

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Chemical Structure| 78755-81-4 同义名 : Ro 15-1788;Ro 1722;Flumazenil, Flumazepil, Anexate, Romazicon, Lanexat, Ro 15-1788, Ro 15 1788, Ro 151788;Ro 41-8157
CAS号 : 78755-81-4
货号 : A423241
分子式 : C15H14FN3O3
纯度 : 95%
分子量 : 303.288
MDL号 : -
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 18 mg/mL(59.35 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • GABAA receptor
描述 Flumazenil, an imidazobenzodiazepine derivative, is an antagonist of the GABA/benzodiazepines receptor complex that might play a role in the treatment of hepatic encephalopathy[3]. Flumazenil can antagonize the hypnotic and sedative effects of benzodiazepines at gamma-amino butyric acid receptors. Flumazenil could be considered in cases in which quick recovery is required and should be administered intravenously in small, incremental doses[4]. Intravenous antagonist doses of 0.2 mg followed by 0.1 mg/min to a total dose of 1 mg have produced significant results in reversing benzodiazepine sedation. As much as 5 mg of flumazenil have been necessary when treating benzodiazepine or mixed-agent intoxications. Flumazenil is well tolerated locally as well as systemically[5]. Because flumazenil appears to be specific in its antagonism of benzodiazepine-induced respiratory and CNS depression, it could be used empirically to confirm or exclude a role of benzodiazepines in the generation of mental status changes in the setting of overdose or coma of unknown origin[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.30mL

0.66mL

0.33mL

16.49mL

3.30mL

1.65mL

32.97mL

6.59mL

3.30mL
参考文献

[1]Belzung C, Le Guisquet AM, et al. Flumazenil induces benzodiazepine partial agonist-like effects in BALB/c but not C57BL/6 mice. Psychopharmacology (Berl). 2000 Jan;148(1):24-32.

[2]Hoffman EJ, Warren EW. Flumazenil: a benzodiazepine antagonist. Clin Pharm. 1993 Sep;12(9):641-56; quiz 699-701.

[3]Reyes D, Barrera F. Is flumazenil an alternative for the treatment of hepatic encephalopathy? Medwave. 2017 Dec 26;17(9):e7113.

[4]Mizuno J. [Flumazenil]. Masui. 2013 Jan;62(1):10-8.

[5]Karavokiros KA, Tsipis GB. Flumazenil: a benzodiazepine antagonist. DICP. 1990 Oct;24(10):976-81

[6]Votey SR, Bosse GM, Bayer MJ, Hoffman JR. Flumazenil: a new benzodiazepine antagonist. Ann Emerg Med. 1991 Feb;20(2):181-8