keyword
MENU ▼
Read by QxMD icon Read
search

flumazenil

keyword
https://www.readbyqxmd.com/read/28807671/selective-inhibition-of-extra-synaptic-%C3%AE-5-gabaa-receptors-by-s44819-a-new-therapeutic-agent
#1
Lori-An Etherington, Balázs Mihalik, Adrienn Pálvölgyi, István Ling, Katalin Pallagi, Szabolcs Kertész, Péter Varga, Ben G Gunn, Adam R Brown, Matthew R Livesey, Olivia Monteiro, Delia Belelli, József Barkóczy, Michael Spedding, István Gacsályi, Ferenc A Antoni, Jeremy J Lambert
In the mammalian central nervous system (CNS) GABAA receptors (GABAARs) mediate neuronal inhibition and are important therapeutic targets. GABAARs are composed of 5 subunits, drawn from 19 proteins, underpinning expression of 20-30 GABAAR subtypes. In the CNS these isoforms are heterogeneously expressed and exhibit distinct physiological and pharmacological properties. We report the discovery of S44819, a novel tricyclic oxazolo-2,3-benzodiazepine-derivative, that selectively inhibits α5-subunit-containing GABAARs (α5-GABAARs)...
August 12, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28798689/high-resolution-uhplc-ms-metabolomics-and-sedative-anxiolytic-effects-of-latua-pubiflora-a-mystic-plant-used-by-mapuche-amerindians
#2
Eliana L Sánchez-Montoya, Marco A Reyes, Joel Pardo, Juana Nuñez-Alarcón, José G Ortiz, Juan C Jorge, Jorge Bórquez, Andrei Mocan, Mario J Simirgiotis
Latua pubiflora (Griseb) Phil. Is a native shrub of the Solanaceae family that grows freely in southern Chile and is employed among Mapuche aboriginals to induce sedative effects and hallucinations in religious or medicine rituals since prehispanic times. In this work, the pentobarbital-induced sleeping test and the elevated plus maze test were employed to test the behavioral effects of extracts of this plant in mice. The psychopharmacological evaluation of L. pubiflora extracts in mice determined that both alkaloid-enriched as well as the non-alkaloid extracts produced an increase of sleeping time and alteration of motor activity in mice at 150 mg/Kg...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28796283/flumazenil-versus-placebo-or-no-intervention-for-people-with-cirrhosis-and-hepatic-encephalopathy
#3
REVIEW
Ee Teng Goh, Mette L Andersen, Marsha Y Morgan, Lise Lotte Gluud
BACKGROUND: Hepatic encephalopathy is a common complication of cirrhosis which results in poor brain functioning. The spectrum of changes associated with hepatic encephalopathy ranges from the clinically 'indiscernible' or minimal hepatic encephalopathy to the clinically 'obvious' or overt hepatic encephalopathy. Flumazenil is a synthetic benzodiazepine antagonist with high affinity for the central benzodiazepine recognition site. Flumazenil may benefit people with hepatic encephalopathy through an indirect negative allosteric modulatory effect on gamma-aminobutyric acid receptor function...
August 10, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28795023/leptocarpus-disjunctus-prolongs-sleeping-time-and-increases-nonrapid-eye-movement-sleep-with-additional-anxiolytic-capacity
#4
Watchara Damjuti, Thanes Fuangfoo, Chanida Palanuvej, Tingli Li, Nijsiri Ruangrungsi
Leptocarpus disjunctus Mast. (Restionaceae) is an edible plant which has indigenous warnings regarding its side effects which can manifest as dizziness. This study investigated hypnotic and anxiolytic properties using several animal models. Anxiolytic activities were evaluated using locomotor determination by elevated plus-maze test, open-field test, and rotarod performance test. Hypnotic activities were performed using pentobarbital sodium-induced sleeping time test. Sleep architecture and quality were obtained from sleep-wake analysis and nonrapid eye movement (NREM) delta activity using electroencephalography...
July 2017: Journal of Advanced Pharmaceutical Technology & Research
https://www.readbyqxmd.com/read/28777735/evidence-for-the-involvement-of-the-gaba-ergic-pathway-in-the-anticonvulsant-activity-of-the-roots-bark-aqueous-extract-of-anthocleista-djalonensis-a-chev-loganiaceae
#5
Germain Sotoing Taiwe, Arielle Larissa Ndieudieu Kouamou, Armelle Rosalie Mbang Ambassa, Joseph Renaud Menanga, Thierry Bang Tchoya, Paul Desire Djomeni Dzeufiet
BACKGROUND: The root bark of Anthocleista djalonensis A. Chev. (Loganiaceae) is widely used in traditional medicine in Northern Cameroon to treat epilepsy and related conditions, such as migraine, insomnia, dementia, anxiety, and mood disorders. METHODS: To investigate the anticonvulsant effects and the possible mechanisms of this plant, an aqueous extract of Anthocleista djalonensis (AEAD) was evaluated by using animal models of bicuculline-, picrotoxin-, pilocarpine-, and pentylenetetrazole-induced convulsions...
August 4, 2017: Journal of Basic and Clinical Physiology and Pharmacology
https://www.readbyqxmd.com/read/28748168/potentiating-effects-of-perovskia-abrotanoides-karel-on-pentobarbital-induced-sleep
#6
Fatemeh Forouzanfar, Azar Hosseini, Mohammad Sadegh Amiri, Hassan Rakhshandeh
OBJECTIVE: Sleeplessness is the most common sleep disorder. In this study the hypnotic effect of the hydro-alcoholic extract (HAE) of Perovskia abrotanoides Karel. and its water fraction (WF), ethyl acetate fraction (EAF) and n-butanol fraction (NBF) were studied in mice. MATERIALS AND METHODS: The test compounds were administered intraperitoneally to mice 30 min before the administration of sodium pentobarbital (30 mg/kg.). Moreover, the influence of flumazenil on the hypnotic effect of the extracts was evaluated...
May 2017: Avicenna Journal of Phytomedicine
https://www.readbyqxmd.com/read/28745801/flumazenil-versus-placebo-or-no-intervention-for-people-with-cirrhosis-and-hepatic-encephalopathy
#7
REVIEW
Ee Teng Goh, Mette L Andersen, Marsha Y Morgan, Lise Lotte Gluud
BACKGROUND: Hepatic encephalopathy is a common complication of cirrhosis which results in poor brain functioning. The spectrum of changes associated with hepatic encephalopathy ranges from the clinically 'indiscernible' or minimal hepatic encephalopathy to the clinically 'obvious' or overt hepatic encephalopathy. Flumazenil is a synthetic benzodiazepine antagonist with high affinity for the central benzodiazepine recognition site. Flumazenil may benefit people with hepatic encephalopathy through an indirect negative allosteric modulatory effect on gamma-aminobutyric acid receptor function...
July 26, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28740086/novel-molecule-exhibiting-selective-affinity-for-gabaa-receptor-subtypes
#8
Cecilia M Borghese, Melissa Herman, Lawrence D Snell, Keri J Lawrence, Hyun-Young Lee, Donald S Backos, Lauren A Vanderlinden, R Adron Harris, Marisa Roberto, Paula L Hoffman, Boris Tabakoff
Aminoquinoline derivatives were evaluated against a panel of receptors/channels/transporters in radioligand binding experiments. One of these derivatives (DCUK-OEt) displayed micromolar affinity for brain γ-aminobutyric acid type A (GABAA) receptors. DCUK-OEt was shown to be a positive allosteric modulator (PAM) of GABA currents with α1β2γ2, α1β3γ2, α5β3γ2 and α1β3δ GABAA receptors, while having no significant PAM effect on αβ receptors or α1β1γ2, α1β2γ1, α4β3γ2 or α4β3δ receptors...
July 24, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28733205/-dehydrofukinone-modulates-membrane-potential-and-delays-seizure-onset-by-gabaa-receptor-mediated-mechanism-in-mice
#9
Quelen Iane Garlet, Luana da Costa Pires, Laura Hautrive Milanesi, Joseane Righes Marafiga, Bernardo Baldisserotto, Carlos Fernando Mello, Berta Maria Heinzmann
(+)-Dehydrofukinone (DHF), isolated from Nectandra grandiflora (Lauraceae) essential oil, induces sedation and anesthesia by modulation of GABAa receptors. However, no study has addressed whether DHF modulates other cellular events involved in the control of cellular excitability, such as seizure behavior. Therefore, the aim of the present study was to investigate the effect of DHF on cellular excitability and seizure behavior in mice. For this purpose, we used isolated nerve terminals (synaptosomes) to examine the effect of DHF on the plasma membrane potential, the involvement of GABAa receptors and the downstream activation of Ca(2+) mobilization...
July 18, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28730280/evidence-for-the-involvement-of-the-gabaergic-but-not-serotonergic-transmission-in-the-anxiolytic-like-effect-of-bisabolol-in-the-mouse-elevated-plus-maze
#10
Mohaddeseh Abouhosseini Tabari, Mohammad Amir Bagherpour Tehrani
Bisabolol (α-(-)-bisabolol) is a sesquiterpene which is a part of the essential oil of a variety of plants, but its common source is German chamomile. Several bioactivities including anti-inflammatory, anti-nociceptive, and anti-tumor effects were attributed to bisabolol. However, the neuropharmacological properties of bisabolol have not yet been reported. The present study evaluated behavioral effects of bisabolol using elevated plus maze (EPM), open field test (OFT), and rotarod test. Moreover, this study also examined whether the 5-HT1A and GABAA-benzodiazepine receptor systems are involved in the anxiolytic-like effects of bisabolol...
July 20, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28728462/increased-binding-potential-of-brain-adenosine-a-sub-1-sub-receptor-in-chronic-stages-of-patients-with-diffuse-axonal-injury-measured-with-1-methyl-sup-11-sup-c-8-dicyclopropylmethyl-1-methyl-3-propylxanthine-pet-imaging
#11
Shihori Hayashi, Motoki Inaji, Tadashi Nariai, Keiichi Oda, Muneyuki Sakata, Jun Toyohara, Kenji Ishii, Kiichi Ishiwata, Taketoshi Maehara
The positron emission tomography (PET) radioligand for adenosine A <sub>1</sub> receptor (A1R) [1-methyl- <sup>11</sup>C] 8-dicyclopropylmethyl-1-methyl-3-propylxanthine (MPDX) has recently been developed for human brain imaging. In the present study, we evaluated the alteration of the A1R in patients with diffuse axonal injury (DAI) in chronic stage <i>in vivo</i>. Ten patients with DAI (7 men and 3 women) were included in this study. Three PET examinations were sequentially performed to measure A1R binding with <sup>11</sup>C-MPDX, glucose metabolism with <sup>18</sup>F-fluorodeoxyglucose (FDG), and central benzodiazepine receptor binding with <sup>11</sup>C-flumazenil (FMZ), decreases of <sup>11</sup>C-FMZ uptake indicate neuronal loss...
July 20, 2017: Journal of Neurotrauma
https://www.readbyqxmd.com/read/28715875/acute-orexigenic-effect-of-agmatine-involves-interaction-between-central-%C3%AE-2-adrenergic-and-gabaergic-receptors
#12
Brijesh Gulabrao Taksande, Omi Sharma, Manish Manohar Aglawe, Mayur Bhimrao Kale, Dinesh Yugraj Gawande, Milind Janraoji Umekar, Nandkishor Ramdas Kotagale
Agmatine and GABA have been abundantly expressed in brain nuclei involved in regulation of energy homeostasis and promoting stimulation of food intake in rodents. However, their mutual interaction, if any, in the elicitation of feeding behavior is largely remains unclear. The current study provides experimental evidence for the possible interaction of agmatine, adrenergic and GABAergic systems in stimulation of feeding in satiated rats. Satiated rats fitted with intracerebroventricular (i.c.v.) cannulae and were administered agmatine, alone or jointly with (a) GABAA receptor agonist, muscimol, diazepam or antagonist bicuculline and flumazenil, GABAA positive modulator, allopregnanolone or negative modulator of GABAA receptor, dehydroepiandrosterone (b) In view of the high affinity of agmatine for α2-adrenoceptors and the close association between α2-adrenoceptors and GABAergic system, the effect of their modulators on feeding elicited by agmatine/GABAergic agonists were also examined...
September 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28708699/flumazenil-for-mixed-drug-overdose
#13
Rukma Parthvi, Sunil Mehra
No abstract text is available yet for this article.
July 6, 2017: American Journal of Therapeutics
https://www.readbyqxmd.com/read/28654794/preclinical-evidence-of-the-anxiolytic-and-sedative-like-activities-of-tagetes-erecta-l-reinforces-its-ethnobotanical-approach
#14
Gimena Pérez-Ortega, Guadalupe Esther Angeles-López, Arturo Argueta-Villamar, María Eva González-Trujano
Morelos State is one of the regions of Mexico where several plant species are used in traditional medicine. Species from Tagetes genus (Asteraceae) are reported as useful in infusion to treat stomachache and intestinal diseases, but also as tranquilizers. In this study, medicinal uses of T. erecta including its depressant effect on the central nervous system (CNS) were explored by interviewing healers and merchants of local markets of Morelos State, and by investigation of the phytochemical and pharmacological tranquilizing properties...
September 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28645783/maerua-angolensis-stem-bark-extract-reverses-anxiety-and-related-behaviours-in-zebrafish-involvement-of-gabaergic-and-5-ht-systems
#15
Charles Kwaku Benneh, Robert Peter Biney, Priscilla Kolibea Mante, Augustine Tandoh, Donatus Wewura Adongo, Eric Woode
ETHNOPHARMACOLOGICAL RELEVANCE: Maerua angolensis DC (Capparaceae) has been employed in the management of several central nervous system (CNS) disorders including anxiety. This study evaluated the anxiolytic effects of the petroleum ether/ethyl acetate fraction stem bark extract and its possible mechanism(s) using zebrafish anxiety models. METHODS: Adult zebrafish, tested in the novel tank and light dark tests, have shown by previous authors to be sensitive to the anxiolytic effects of known anxiolytic drugs...
June 20, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28631142/parametric-imaging-of-11-c-flumazenil-binding-in-the-rat-brain
#16
Isadora Lopes Alves, David Vállez Vállez García, Andrea Parente, Janine Doorduin, Ana Maria Marques da Silva, Michel Koole, Rudi Dierckx, Antoon Willemsen, Ronald Boellaard
PURPOSE: This study evaluates the performance of several parametric methods for assessing [(11)C]flumazenil binding distribution in the rat brain. PROCEDURES: Dynamic (60 min) positron emission tomography data with metabolite-corrected plasma input function were retrospectively analyzed (male Wistar rats, n = 10). Distribution volume (V T) images were generated from basis function method (BFM), Logan graphical analysis (Logan), and spectral analysis (SA). Using the pons as pseudo-reference tissue, binding potential (BP ND and DVR-1) images were obtained from receptor parametric imaging algorithms (RPM and SRTM2) and reference Logan (RLogan)...
June 19, 2017: Molecular Imaging and Biology: MIB: the Official Publication of the Academy of Molecular Imaging
https://www.readbyqxmd.com/read/28613124/low-risk-of-seizures-with-slow-flumazenil-infusion-and-routine-anticonvulsant-prophylaxis-for-high-dose-benzodiazepine-dependence
#17
Stefano Tamburin, Marco Faccini, Rebecca Casari, Angela Federico, Laura Morbioli, Enrica Franchini, Luigi Giuseppe Bongiovanni, Fabio Lugoboni
High-dose benzodiazepine (BZD) dependence represents an emerging and under-reported addiction phenomenon and is associated with reduced quality of life. To date there are no guidelines for the treatment of high-dose BZD withdrawal. Low-dose slow flumazenil infusion was reported to be effective for high-dose BZD detoxification, but there is concern about the risk of convulsions during this treatment. We evaluated the occurrence of seizures in 450 consecutive high-dose BZD dependence patients admitted to our unit from April 2012 to April 2016 for detoxification with low-dose slow subcutaneous infusion of flumazenil associated with routine anticonvulsant prophylaxis...
June 1, 2017: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/28587936/intra-hippocampal-microinjection-of-oxytocin-produced-antiepileptic-effect-on-the-pentylenetetrazol-induced-epilepsy-in-rats
#18
Amir Erfanparast, Esmaeal Tamaddonfard, Farzin Henareh-Chareh
BACKGROUND: In addition to its role as a circulating hormone, oxytocin can also act as a neurotransmitter and a neuromodulator within the brain. In this study, we investigated the intra-hippocampal effect of oxytocin on an experimental seizure model induced by pentylenetetrazole (PTZ) in rats. We also used atosiban (oxytocin antagonist), diazepam and flumazenil (gamma-aminobutyric acid or GABA-benzodiazepine receptor agonist and antagonist, respectively) to clarify the involved mechanism...
March 12, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28585447/anticonvulsant-effects-of-aerial-parts-of-verbena-officinalis-extract-in-mice-involvement-of-benzodiazepine-and-opioid-receptors
#19
Amir Rashidian, Fatemeh Kazemi, Saeed Mehrzadi, Ahmad Reza Dehpour, Shahram Ejtemai Mehr, Seyed Mahdi Rezayat
To evaluate the anticonvulsant activity of the aerial parts of Verbena officinalis used traditionally by local Iranians for the treatment of convulsion. The anticonvulsant activity of the extract was assessed in pentylenetetrazole (PTZ) and maximal electroshock (MES) induced seizures in mice. Diazepam was used as reference drug. In addition, for investigating the mechanism of V officinalis in PTZ model, flumazenil and naloxone were injected before V officinalis. The extract showed no toxicity and significantly increased the period taken before the onset and decreased the duration of the seizures induced by PTZ...
January 1, 2017: Journal of Evidence-based Complementary & Alternative Medicine
https://www.readbyqxmd.com/read/28577050/anticonvulsive-activity-of-1s-verbenone-involving-rna-expression-of-bdnf-cox-2-and-c-fos
#20
Cynthia Germoglio Farias de Melo, Paula Regina Rodrigues Salgado, Diogo Vilar da Fonsêca, Renan Marinho Braga, Marcelo Ricardo Dutra Caldas Filho, Ingrid Eulália Vieira de Farias, Hilzeth de Luna Freire Pessôa, Eleonidas Moura Lima, Ian Porto Gurgel do Amaral, Damião Pergentino de Sousa, Reinaldo Nóbrega de Almeida
(1S)-(-)-verbenone (VRB) is a monoterpene present in the essential oils of many plants which has shown therapeutic effect; however, its anticonvulsant activity has not yet been evaluated. The present work sought to investigate the anticonvulsant activity of VRB using pilocarpine and pentylenetetrazole-induced seizure testing; seeking also probable mechanisms of action. VRB caused no significant changes in motor coordination. Also, no significant data was observed in the pilocarpine-induced seizure tests. In the PTZ-induced seizures test, VRB showed anticonvulsant activity at doses of 200 mg/kg i...
June 2, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
keyword
keyword
49300
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"