Flumazenil - CAS 78755-81-4
Catalog number: 78755-81-4
Category: Inhibitor
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GABA Receptor
Flumazenil is a GABAA receptor antagonist and the only GABAA receptor antagonist on the market today.
Flumazenil, Flumazepil, Anexate, Romazicon, Lanexat, Ro 15-1788, Ro 15 1788, Ro 151788
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1.Design of Infusion Schemes for Neuroreceptor Imaging: Application to [(11)C]Flumazenil-PET Steady-State Study.
Feng L1, Svarer C1, Madsen K1, Ziebell M1, Dyssegaard A1, Ettrup A1, Hansen HD1, Lehel S2, Yndgaard S3, Paulson OB4, Knudsen GM5, Pinborg LH6. Biomed Res Int. 2016;2016:9132840. doi: 10.1155/2016/9132840. Epub 2016 Mar 31.
This study aims at developing a simulation system that predicts the optimal study design for attaining tracer steady-state conditions in brain and blood rapidly. Tracer kinetics was determined from bolus studies and used to construct the system. Subsequently, the system was used to design inputs for bolus infusion (BI) or programmed infusion (PI) experiments. Steady-state quantitative measurements can be made with one short scan and venous blood samples. The GABAA receptor ligand [(11)C]Flumazenil (FMZ) was chosen for this purpose, as it lacks a suitable reference region. Methods. Five bolus [(11)C]FMZ-PET scans were conducted, based on which population-based PI and BI schemes were designed and tested in five additional healthy subjects. The design of a PI was assisted by an offline feedback controller. Results. The system could reproduce the measurements in blood and brain. With PI, [(11)C]FMZ steady state was attained within 40 min, which was 8 min earlier than the optimal BI (B/I ratio = 55 min).
2.The effects of intravenous aminophylline on level of consciousness in acute intentional benzodiazepines poisoning in comparison to flumazenil.
Aghabiklooei A1, Sangsefidi J2. Hum Exp Toxicol. 2016 May 2. pii: 0960327116646619. [Epub ahead of print]
AIM: Acute intentional benzodiazepine poisoning is marked by a significant loss of consciousness, aspiration pneumonia, and increased rates of mortality and morbidity, especially in older patients with underlying heart or lung disease. These patients may need flumazenil to reverse the respiratory effects of benzodiazepines. The positive effects of aminophylline on respiration and neonatal apnea improvement have been shown previously. However, its possible effects on increasing the level of consciousness have never been evaluated.
3.Determination of flumazenil in serum by liquid chromatography-mass spectrometry: Application to kinetics study in acute diazepam overdose.
Djordjević S, Jović-Stosić J, Kilibarda V, Segrt Z, Perković-Vukcević N. Vojnosanit Pregl. 2016 Feb;73(2):146-51.
BACKGOUND/AIM: Flumazenil is benzodiazepine receptor antagonist. It has been studied for a various indications, including reversal of sedation after surgery or diagnostic procedures, awakening of comatose patients in benzodiazepine overdose, or for symptomatic treatment of hepatic encephalopathy. Some drugs, like theophylline, may prolong its elimination half-life. Considering the long half-life of diazepam and its metabolites, concomitant use of theophylline may reduce the need for repeated dosing of flumazenil in patients with acute diazepam poisoning. The aim of this study was to introduce a reliable and accurate method for determining the concentration of flumazenil after therapeutic application in patients with acute poisoning, and using that method to assess whether the kinetics of flumazenil change in the presence of aminophylline (combination of theophylline and ethylenediamine in a 2:1 ratio) applied as concomitant therapy.
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CAS 78755-81-4 Flumazenil

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