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Submit ReviewFlumazenil
说明： Benzodiazepine antagonist
别名： Ro 15-1788
化学名： 8-Fluoro-5,6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylic acid, ethyl ester
纯度： ≥99% (HPLC)
生物活性 for Flumazenil
Flumazenil is a benzodiazepine antagonist, non-selective for α1, α2, α3 or α5-containing GABAA receptors. Centrally active upon systemic administration in vivo. Also inhibits repressor element-1 silencing transcription factor (REST) by targeting degradation.
化合物库 for Flumazenil
Flumazenil is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. 了解 Tocris 化合物库的更多信息。
技术数据 for Flumazenil
| 分子量 | 303.29 |
| 公式 | C15H14FN3O3 |
| 储存 | Store at +4°C |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 78755-81-4 |
| PubChem ID | 3373 |
| InChI Key | OFBIFZUFASYYRE-UHFFFAOYSA-N |
| Smiles | CCOC(=O)C1=C2CN(C)C(=O)C3=CC(F)=CC=C3N2C=N1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Flumazenil
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 25 |
制备储备液 for Flumazenil
以下数据基于产品分子量 303.29。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.25 mM | 13.19 mL | 65.94 mL | 131.89 mL |
| 1.25 mM | 2.64 mL | 13.19 mL | 26.38 mL |
| 2.5 mM | 1.32 mL | 6.59 mL | 13.19 mL |
| 12.5 mM | 0.26 mL | 1.32 mL | 2.64 mL |
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产品说明书 for Flumazenil
参考文献 for Flumazenil
参考文献是支持产品生物活性的出版物。
Atack et al (1999) Regional differences in the inhibition of mouse in vivo [3H]Ro 15-1788 binding reflect selectivity for α1 versus α2 and α3 subunit-containing GABAA receptors. Neuropsychopharmacology 20 255 PMID: 10063485
Dobl (1999) New insights into the mechanism of action of hypnotics. J.Psychopharmacol. 13 S11 PMID: 10667451
Polc et al (1981) Electrophysiological studies on the specific benzodiazepine antagonist Ro 15-1788. Naunyn Schmiedebergs Arch.Pharmacol. 316 317 PMID: 7196507
If you know of a relevant reference for Flumazenil, please let us know.
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关键词: Flumazenil, Flumazenil supplier, Benzodiazepine, antagonists, GABAA, Receptors, Ro151788, repressor, element-1, silencing, transcription, factor, REST, inhibitors, inhibits, Ro, 15-1788, Other, Transcription, Factors, 1328, Tocris Bioscience
7 篇 Flumazenil 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Flumazenil 的部分引用包括：
Heidelberg et al (2013) SB-205384 is a positive allosteric modulator of recombinant GABAA receptors containing rat α3, α5, or α6 subunit subtypes coexpressed with β3 and γ2 subunits. J Pharmacol Exp Ther 347 235 PMID: 23902941
Carlile et al (2012) An anxiolytic-like effect of hyperbaric oxygen in the mouse light/dark exploration test. Life Sci 90 267 PMID: 22154905
Brodnik et al (2018) Local GABAA receptor mediated suppression of DA release within the nucleus accumbens. ACS Chem Neurosci 17 1978 PMID: 30253088
Zhu (2018) Structure of a human synaptic GABAA receptor. Nature 559 67 PMID: 29950726
Joensuu et al (2014) Gene expression alterations in the cerebellum and granule neurons of Cstb(-/-) mouse are associated with early synaptic changes and inflammation. PLoS One 9 e89321 PMID: 24586687
Leppä et al (2011) Removal of GABA(A) receptor γ2 subunits from parvalbumin neurons causes wide-ranging behavioral alterations. PLoS One 6 e24159 PMID: 21912668
Linden et al (2011) Ro 15-4513 Antagonizes Alcohol-Induced Sedation in Mice Through αβγ2-type GABA(A) Receptors. Front Neurosci 5 3 PMID: 21270945
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Flumazenil 的评论
平均评分: 5 (基于 2 条评论。)
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Antagonism of Flumazenil to effects of Phenazepam.
By
Anonymous on 04/14/2020
分析类型： In Vitro
种属： Other
Flumazenil (FMZ) was used to block action of other benzodiazepine ligand of GABA-A receptor (Phenazepam, PNZ) on decay kinetics of spontaneous inhibitory currents recorded from brain neurons of Prussian carp (Carassius gibelio). FMZ demonstrated competitive antagonism to PNZ in this research, both in vivo (behavioral tests) and in vitro (whole-cell voltage-clamp recordings, see example illustration).
Soluble in DMSO, but requires sonication.
Flumazenil and in vivo chloride signals.
By
Anonymous on 05/23/2019
分析类型： In Vivo
种属： Mouse
used with fiber photometry to validate a chloride sensor in vivo. response to footshock was measured at baseline and then at 15 min intervals post injection
injected 15mg/kg i.p at a concentration of.8mg/ml in 5% DMSO in saline
该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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