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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
#1
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
#2
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
#3
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
#4
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
#5
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
#6
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
https://www.readbyqxmd.com/read/28551554/antihyperalgesic-activity-of-a-mexicanolide-isolated-from-swietenia-humilis-extract-in-nicotinamide-streptozotocin-hyperglycemic-mice
#7
Berenice Ovalle-Magallanes, Myrna Déciga-Campos, Rachel Mata
Swietenia humilis Zucc. (Meliaceae) seeds are used in Mexico for the treatment of type 2 diabetes mellitus. Mexicanolides are the main hypoglycemic and antihyperglycemic compounds of the species. This study was conducted to investigate the antihyperalgesic effect of an aqueous extract of the seeds of Swietenia humilis (SHAE) and of mexicanolide 2-hydroxy-destigloyl-6-deoxyswietenine acetate (1), using the formalin test in mice. The antihyperalgesic actions of SHAE and mexicanolide 1, as well as its possible transductional activity, were assessed in nicotinamide-streptozotocin (NA-STZ) hyperglycemic mice...
August 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28528187/anticonvulsant-activity-of-pseudospondias-microcarpa-a-rich-engl-hydroethanolic-leaf-extract-in-mice-the-role-of-excitatory-inhibitory-neurotransmission-and-nitric-oxide-pathway
#8
Donatus W Adongo, Priscilla K Mante, Kennedy K E Kukuia, Robert P Biney, Eric Boakye-Gyasi, Charles K Benneh, Elvis O Ameyaw, Eric Woode
ETHNOPHARMACOLOGICAL RELEVANCE: Pseudospondias microcarpa (A. Rich) Engl. is a plant used for managing various diseases including central nervous system disorders. AIM OF THE STUDY: This study explored the anticonvulsant activity of P. microcarpa hydroethanolic leaf extract (PME) as well as possible mechanism(s) of action in animal models. METHODS: Effects of PME was assessed in electroconvulsive (the maximal electroshock and 6-Hz seizures) and chemoconvulsive (pentylenetetrazole-, picrotoxin-, isoniazid-, 4-aminopyridine-, and strychnine-induced seizures) models of epilepsy...
May 17, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28502940/pet-imaging-of-18-f-fdg-11-c-methionine-11-c-flumazenil-and-11-c-4dst-in-progressive-multifocal-leukoencephalopathy
#9
Kenji Ishibashi, Yoshiharu Miura, Ken Matsumura, Yusuke Kanemasa, Kazuo Nakamichi, Masayuki Saijo, Jun Toyohara, Kenji Ishii
The use of positron emission tomography (PET) imaging in progressive multifocal leukoencephalopathy (PML) has rarely been reported. We herein report a set of PET images in a 63-year-old patient with PML. In PML lesions, the uptake of (18)F-fluorodeoxyglucose, (11)C-methionine, (11)C-flumazenil, and [methyl-(11)C]4'-thiothymidine was decreased, increased, decreased, and unchanged, respectively. These results suggest that glucose metabolism decreased, protein synthesis increased, neuronal integrity decreased, and the DNA synthesis and cellular proliferation of host cells were not activated in PML lesions...
2017: Internal Medicine
https://www.readbyqxmd.com/read/28482271/usefulness-of-stereoeeg-based-tailored-surgery-for-medial-temporal-lobe-epilepsy-preliminary-results-in-11-patients
#10
Yuichi Kubota, Taku Ochiai, Tomokatsu Hori, Takakazu Kawamata
OBJECTIVE: Surgical options for medial temporal lobe epilepsy (MTLE) include anterior temporal lobectomy (ATL) and selective amygdalohippocampectomy (SAH). Optimal criteria for choosing the appropriate surgical approach remain uncertain. This article reports 11 consecutive cases in which electrophysiological findings of stereoelectroencephalography (SEEG) were used to determine the optimal surgical approach. PATIENTS AND METHODS: Eleven consecutive patients with MTLE underwent SEEG evaluation and were placed in either the medial or the medial+lateral group based on the findings...
July 2017: Clinical Neurology and Neurosurgery
https://www.readbyqxmd.com/read/28436443/curcumol-allosterically-modulates-gaba-a-receptors-in-a-manner-distinct-from-benzodiazepines
#11
Yan-Mei Liu, Hui-Ran Fan, Jing Ding, Chen Huang, Shining Deng, Tailin Zhu, Tian-Le Xu, Wei-Hong Ge, Wei-Guang Li, Fei Li
Inhibitory A type γ-aminobutyric acid receptors (GABAARs) play a pivotal role in orchestrating various brain functions and represent an important molecular target in neurological and psychiatric diseases, necessitating the need for the discovery and development of novel modulators. Here, we show that a natural compound curcumol, acts as an allosteric enhancer of GABAARs in a manner distinct from benzodiazepines. Curcumol markedly facilitated GABA-activated currents and shifted the GABA concentration-response curve to the left in cultured hippocampal neurons...
April 24, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28435427/novel-4-thiazolidinone-derivatives-as-agonists-of-benzodiazepine-receptors-design-synthesis-and-pharmacological-evaluation
#12
Mehrdad Faizi, Reza Jahani, Seyed Abbas Ebadi, Sayyed Abbas Tabatabai, Elham Rezaee, Mehrnaz Lotfaliei, Mohsen Amini, Ali Almasirad
A new series of 4-chloro-N-(2-(substitutedphenyl)-4-oxothiazolidin-3-yl)-2-phenoxybenzamide derivatives were designed, synthesized and biologically evaluated as anticonvulsant agents. The designed compounds have the main essential functional groups for binding to the benzodiazepine receptors and 4-thiazolidinone ring as an anticonvulsant pharmacophore. Some of the new synthesized compounds showed considerable anticonvulsant activity in electroshock and pentylenetetrazole-induced lethal convulsion tests. Compound 5i, 4-chloro-N-(2-(4-methoxyphenyl)-4-oxothiazolidin-3-yl)-2-phenoxybenzamide, with the best activity was selected for evaluation of other benzodiazepine pharmacological effects...
2017: EXCLI journal
https://www.readbyqxmd.com/read/28432674/partial-volume-correction-of-brain-pet-studies-using-iterative-deconvolution-in-combination-with-hypr-denoising
#13
Sandeep S V Golla, Mark Lubberink, Bart N M van Berckel, Adriaan A Lammertsma, Ronald Boellaard
BACKGROUND: Accurate quantification of PET studies depends on the spatial resolution of the PET data. The commonly limited PET resolution results in partial volume effects (PVE). Iterative deconvolution methods (IDM) have been proposed as a means to correct for PVE. IDM improves spatial resolution of PET studies without the need for structural information (e.g. MR scans). On the other hand, deconvolution also increases noise, which results in lower signal-to-noise ratios (SNR). The aim of this study was to implement IDM in combination with HighlY constrained back-PRojection (HYPR) denoising to mitigate poor SNR properties of conventional IDM...
December 2017: EJNMMI Research
https://www.readbyqxmd.com/read/28427112/acute-encephalopathy-in-a-2-year-old-pot-bellied-pig-following-accidental-intoxication-with-clonazepam
#14
Emilie L Setlakwe, Amy L Johnson
OBJECTIVE: To describe a case of successful management of clonazepam toxicity causing encephalopathy in a pot-bellied pig. CASE SUMMARY: A 2-year-old female pot-bellied pig weighing 13.5 kg was presented for evaluation of clinical signs of acute encephalopathy. Based on the animal's history and clinical signs, a tentative diagnosis of benzodiazepine (BZP) intoxication was made. The results of a urinary drug screening test designed to detect illicit substances in human urine indicated benzodiazepine exposure...
May 2017: Journal of Veterinary Emergency and Critical Care
https://www.readbyqxmd.com/read/28424803/use-of-a-flumazenil-infusion-to-treat-chlordiazepoxide-toxicity
#15
I R Wallace, E C Campbell, M Trimble
"Alcohol detox" is a common presentation to acute medical services and is usually managed via standardised guidelines and protocols. We present a case of chlordiazepoxide toxicity, requiring repeated bolus doses and subsequently 24 hours of an intravenous infusion of flumazenil in response to guideline directed management of an alcohol withdrawal state. The use of prolonged flumazenil infusions to treat benzodiazepine toxicity is infrequently described. Chlordiazepoxide is metabolised in the hepatic microsomal pathway and hepatic impairment can lead to accumulation of toxic metabolites, which may have been the explanation for toxicity in this case...
2017: Acute Medicine
https://www.readbyqxmd.com/read/28424564/new-developments-in-the-management-of-narcolepsy
#16
REVIEW
Vivien C Abad, Christian Guilleminault
Narcolepsy is a life-long, underrecognized sleep disorder that affects 0.02%-0.18% of the US and Western European populations. Genetic predisposition is suspected because of narcolepsy's strong association with HLA DQB1*06-02, and genome-wide association studies have identified polymorphisms in T-cell receptor loci. Narcolepsy pathophysiology is linked to loss of signaling by hypocretin-producing neurons; an autoimmune etiology possibly triggered by some environmental agent may precipitate hypocretin neuronal loss...
2017: Nature and Science of Sleep
https://www.readbyqxmd.com/read/28411234/phenotype-of-gaba-transaminase-deficiency
#17
REVIEW
Mary Kay Koenig, Ryan Hodgeman, James J Riviello, Wendy Chung, Jennifer Bain, Claudia A Chiriboga, Kazushi Ichikawa, Hitoshi Osaka, Megumi Tsuji, K Michael Gibson, Penelope E Bonnen, Phillip L Pearl
OBJECTIVE: We report a case series of 10 patients with γ-aminobutyric acid (GABA)-transaminase deficiency including a novel therapeutic trial and an expanded phenotype. METHODS: Case ascertainment, literature review, comprehensive evaluations, and long-term treatment with flumazenil. RESULTS: All patients presented with neonatal or early infantile-onset encephalopathy; other features were hypotonia, hypersomnolence, epilepsy, choreoathetosis, and accelerated linear growth...
May 16, 2017: Neurology
https://www.readbyqxmd.com/read/28406873/investigation-of-the-anxiolytic-and-antidepressant-effects-of-curcumin-a-compound-from-turmeric-curcuma-longa-in-the-adult-male-sprague-dawley-rat
#18
Tomás Eduardo Ceremuga, Katie Helmrick, Zachary Kufahl, Jesse Kelley, Brian Keller, Fabiola Philippe, James Golder, Gina Padrón
As the use of herbal medications continues to increase in America, the potential interaction between herbal and prescription medications necessitates the discovery of their mechanisms of action. The purpose of this study was to investigate the anxiolytic and antidepressant effects of curcumin, a compound from turmeric (Curcuma longa), and its effects on the benzodiazepine site of the γ-aminobutyric acid receptor A (GABAA) receptor. Utilizing a prospective, between-subjects group design, 55 male Sprague-Dawley rats were randomly assigned to 1 of the 5 intraperitoneally injected treatment groups: vehicle, curcumin, curcumin + flumazenil, midazolam, and midazolam + curcumin...
May 2017: Holistic Nursing Practice
https://www.readbyqxmd.com/read/28391167/ameliorative-potential-of-colebrookea-oppositifolia-methanolic-root-extract-against-experimental-models-of-epilepsy-possible-role-of-gaba-mediated-mechanism
#19
Gollapalle Lakshminarayanashastry Viswanatha, Marikunte V Venkataranganna, Nunna Bheema Lingeswara Prasad
BACKGROUND: Colebrookea oppositifolia Smith is one of the commonly used plants to treat epilepsy by various folk medicine communities like nomadic Gujjars, Tharu and Bhoxa in sub-Himalayan regions of India. PURPOSE: The present study was undertaken to evaluate the anticonvulsant activity of roots of Colebrookea oppositifolia using various experimental models of epilepsy in mice. METHODS: Petroleum ether extract of roots of C. Oppositifolia (PeCO), methanolic eCO (MeCO) and aqueous eCO (AeCO) was initially evaluated in six-hertz-seizure test in mice, the effective extract was further evaluated against maximal electroshock (MES) and pentylenetetrazole (PTZ) models in mice...
June 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28364664/contribution-of-neuroinflammation-to-changes-in-11-c-flumazenil-binding-in-the-rat-brain-evaluation-of-the-inflamed-pons-as-reference-tissue
#20
Andrea Parente, David Vállez García, Alexandre Shoji, Isadora Lopes Alves, Bram Maas, Rolf Zijlma, Rudi Ajo Dierckx, Carlos A Buchpiguel, Erik Fj de Vries, Janine Doorduin
INTRODUCTION: [(11)C]Flumazenil is a well-known PET tracer for GABAA receptors and is mainly used as an imaging biomarker for neuronal loss. Recently, GABAA receptors on immune cells have been investigated as target for modulation of inflammation. Since neuronal loss is often accompanied by neuroinflammation, PET imaging with [(11)C]flumazenil is potentially affected by infiltrating immune cells. This may also compromise the validity of using the pons as reference tissue in quantitative pharmacokinetic analysis...
June 2017: Nuclear Medicine and Biology
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