CAS:78755-81-4
Storage:Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:≥99%
Appearance:White to off-white Solid
Flumazenil 是一种有竞争性的 GABAA receptor 拮抗剂。
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FlumazenilCAS:78755-81-4
Storage:Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:≥99%
Appearance:White to off-white Solid
CAS | 78755-81-4 |
Chinese Name | 氟马西尼 |
English Name | Flumazenil |
Synonyms | RO 15-1788 |
Molecular Formula | C15H14FN3O3 |
Molecular Weight | 303.29 |
Solubility | Soluble in DMSO |
Purity | ≥99% |
Appearance | White to off-white Solid |
Storage | Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year |
EC | EINECS 616-650-9 |
MDL | MFCD00242764 |
SMILES | O=C(C1=C2CN(C(C3=CC(F)=CC=C3N2C=N1)=O)C)OCC |
InChIKey | OFBIFZUFASYYRE-UHFFFAOYSA-N |
InChI | InChI=1S/C15H14FN3O3/c1-3-22-15(21)13-12-7-18(2)14(20)10-6-9(16)4-5-11(10)19(12)8-17-13/h4-6,8H,3,7H2,1-2H3 |
PubChem CID | 3373 |
Target Point | GABA Receptor |
Passage | Neuronal Signaling;GPCR & G Protein |
Background | Flumazenil is a competitive GABAA receptor antagonist. |
Biological Activity | Flumazenil 是一种有竞争性的 GABAA receptor 拮抗剂,用于治疗苯二氮类药物过量问题。[1-5] |
In Vivo | 氟马西尼与中枢苯二氮卓受体相互作用,以拮抗或逆转苯二氮卓类激动剂和反向激动剂的行为,神经和电生理作用。氟马西尼在肝性脑病中有一定的益处,但在进行精心设计的临床试验之前,必须将肝性脑病视为氟马西尼的研究指征。氟马西尼已经被证明可以逆转单独使用苯二氮卓类药物或苯二氮卓类药物与其他药物联合使用引起的镇静作用,但是当怀疑使用环状抗抑郁药时,不应该使用它[1]。氟马西尼(1 mg/kg)在升高的迷宫和光/暗试验中测试的BALB/c小鼠中诱导强烈的抗焦虑作用[2]。氟马西尼(10 mg/kg)可有效预防大鼠中allopregnanolone的减少[3]。氟马西尼(5-20mg/kg)拮抗地西泮的抗惊厥和不良反应,但不影响小鼠的GYKI 52466。氟马西尼在MES模型中略微降低了NBQX的抗惊厥活性,但在PTZ试验中没有[4]。氟马西尼(3.0 mg/kg)可阻止慢性乙醇治疗的退出,从而减少开放臂时间和开放臂进入百分比[5]。 |
Animal Experiment | 在实验测试前20分钟腹腔注射氟马西尼,体积为10mL/kg体重。用树脂玻璃覆盖的两个聚氯乙烯盒(20×20×14cm)通过不透明的塑料通道(5×7×10cm)连接。其中一个盒子变暗了。 100瓦的台灯在另一个箱子上方40厘米处的灯光提供了唯一的室内照明。选择该光水平(300勒克斯)是为了避免在对照动物的点亮盒中(时间焦虑行为的测量)中及时检测到应变差异。实际上,在先前的实验中,BALB/c小鼠仅在高光条件下与C57BL/6不同。受试者在1400至1700小时之间的5分钟内进行单独测试。将小鼠放在点亮的盒子中以开始测试。在隧道中的第一个条目之后记录在点亮的框中花费的时间以及从暗盒到点亮的盒子的过渡的数量。 |
Data Literature Source | [1]. Hoffman EJ,et al. Flumazenil: a benzodiazepine antagonist. Clin Pharm. 1993 Sep;12(9):641-56; quiz 699-701. [2]. Belzung C,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. [3]. Fernandez-Guasti A,et al. Flumazenil blocks the anxiolytic action of allopregnanolone. Eur J Pharmacol. 1995 Jul 25;281(1):113-5. [4]. Loscher W,et al. Effects of the non-NMDA antagonists NBQX and the 2,3-benzodiazepine GYKI 52466 on different seizure types in mice: comparison with diazepam and interactions with flumazenil. Br J Pharmacol. 1994 Dec;113(4):1349-57. [5]. Moy SS,et al. Flumazenil blockade of anxiety following ethanol withdrawal in rats. Psychopharmacology (Berl). 1997 Jun;131(4):354-60 |
Unit | Bottle |
Specification | 10mg 50mg 100mg |
Flumazenil 是一种有竞争性的 GABAA receptor 拮抗剂。