Flumazenil

Bentué-Ferrer, Danièle; Bureau, M.; Patat, Alain; Allain, H.

doi:10.1111/j.1527-3458.1996.tb00308.x

Cited by 14 publications

(5 citation statements)

References 130 publications

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“…In this work, the reversal of anxiolysis by pretreatment with Gstn suggests that the anxiolytic effect of the biflavonoid AMT is dependent on serotonergic receptors 5-HT 3A/3B (Figure 7). Flumazenil is an antagonist of benzodiazepine action at GABA A receptors, thus inactivating the anxiolytic effects, sedation and hypnosis of benzodiazepines such as diazepam [28,45]. In this work, the reversal of anxiolysis by pretreatment with flumazenil suggests that the anxiolytic effect of the biflavonoid AMT is dependent on the GABA A receptor (Figure 8).…”

Section: Discussionmentioning

confidence: 61%

An Evaluation of the Anxiolytic Potential of Amentoflavone in Adult Zebrafish Undergoing Alcohol Withdrawal: In Vivo and In Silico Studies

Frota,

da Silva,

Alves

et al. 2024

Receptors

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The constant use of alcoholic beverages can deregulate serotonin levels, affecting neurotransmitters and triggering symptoms of anxiety. In this context, the objective of this work was to evaluate the anxiolytic potential and possible action mechanisms of the natural compound amentoflavone against the deleterious effects caused by alcohol withdrawal on the behavior of adult zebrafish (aZF). The experiments showed that amentoflavone did not change locomotion and did not cause toxicity in aZF during up to 96 h of analysis, with a median lethal concentration (LC50) greater than 1.0 mg/mL. The reversal of anxiety by pretreatment with granisetron suggested that the anxiolytic effect of amentoflavone is dependent on serotonergic 5-HT3A/3B receptors. Furthermore, amentoflavone reversed anxiety due to flumazenil pretreatment, suggesting a dependence on the GABAA receptor. The three concentrations of amentoflavone tested were effective in treating anxiety resulting from alcohol withdrawal. In silico analysis validated the in vivo results, supporting the idea that the interaction of amentoflavone with the protein occurs in a more stable manner than reference compounds. Amid growing interest in natural alternatives to treat anxiety disorders, amentoflavone is a potential candidate for a new anxiolytic compound that acts specifically on the 5HT3A/3B and GABAergic serotonergic pathways.

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Section: Discussionmentioning

confidence: 61%

An Evaluation of the Anxiolytic Potential of Amentoflavone in Adult Zebrafish Undergoing Alcohol Withdrawal: In Vivo and In Silico Studies

Frota,

da Silva,

Alves

et al. 2024

Receptors

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“…Next, we investigated the van Leusen imidazole reaction, [46] to synthesize the fused tetracyclic imidazo-1,5-dibenzothiazepines 4. Fused imidazo-azepines have been reported as selective GABAA receptor antagonist (e. g. Flumazenil), [47] antiviral and antibacterial agents. [48] Satisfyingly, under mild conditions, we were able to get the desired polycyclic thiazepines 4 a-g in good yields (Scheme 3, 22-91 %).…”

Section: Resultsmentioning

confidence: 99%

Dibenzothiazepine Based MCR Chemistry

et al. 2022

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Privileged scaffolds which can unveil unknown territories of the chemical space are constantly prominent. As such, 1,5-dibenzothiazepines not only offer structural diversification but also a very unique binding mode due to their "butterfly" conformation. We provide MCR-based annulations of this scaffold towards three different tetracycles in a straightforward, two-step procedure. We synthesize a library of 30 tetracyclic 1,5tetrazolo-, fused imidazo-and lactam-1,5-dibenzothiazepines with scalable and one-pot procedures. In addition, we obtained single crystal structures of certain derivatives, demonstrating the conformational behavior of the scaffold.

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“…FLU is characterized by short half-life (0.8–1.2 h) ( 30 ) and requires repeated doses or continuous infusion to reverse BZD overdose. In spite of its low lipophilicity, FLU has a large volume of distribution, and its weak binding to plasma proteins explains its rapid distribution.…”

Section: Discussionmentioning

confidence: 99%

Continuous Infusion of Flumazenil in the Management of Benzodiazepines Detoxification

et al. 2021

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An effective approach in the treatment of benzodiazepine (BZD) overdosing and detoxification is flumazenil (FLU). Studies in chronic users who discontinued BZD in a clinical setting suggested that multiple slow bolus infusions of FLU reduce BZD withdrawal symptoms. The aim of this study was to confirm FLU efficacy for reducing BZD withdrawal syndrome by means of continuous elastomeric infusion, correlated to drugs plasma level and patients' compliance.Methods: Seven-day FLU 1 mg/day subcutaneously injected through an elastomeric pump and BZDs lormetazepam, clonazepam, and lorazepam were assessed by HPLC-MS/MS in serum of patients before and after 4 and 7 days of FLU continuous infusion treatment. Changes in withdrawal severity were assessed by using the BZD Withdrawal Scale (BWS).Results: Fourteen patients (mean age ± SD 42.5 ± 8.0 years, 5 male and 9 female), admitted to the hospital for high-dose BZD detoxification, were enrolled in the study. Serum FLU concentrations significantly decreased from 0.54 ± 0.33 ng/ml (mean ± SD) after 4 days of treatment to 0.1 ± 0.2 ng/ml at the end of infusion. Lormetazepam concentrations were 502.5 ± 610.0 ng/ml at hospital admission, 26.2 ± 26.8 ng/ml after 4 days, and 0 at the end of treatment. BWS values decreased during FLU treatment temporal period. FLU was well-tolerated by patients.Conclusions: Elastomeric FLU infusion for BZD detoxification is a feasible administration device to maintain adequate, constant, and tolerated FLU concentrations for reducing BZD withdrawal symptoms.

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Flumazenil

Cited by 14 publications

References 130 publications

An Evaluation of the Anxiolytic Potential of Amentoflavone in Adult Zebrafish Undergoing Alcohol Withdrawal: In Vivo and In Silico Studies

An Evaluation of the Anxiolytic Potential of Amentoflavone in Adult Zebrafish Undergoing Alcohol Withdrawal: In Vivo and In Silico Studies

Dibenzothiazepine Based MCR Chemistry

Continuous Infusion of Flumazenil in the Management of Benzodiazepines Detoxification

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