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https://www.readbyqxmd.com/read/28714785/effects-of-alcohol-on-inhibitory-avoidance-learning-in-zebrafish-danio-rerio
#1
Ricardo Rodrigues Amorim, Priscila Fernandes Silva, Ana Carolina Luchiari
The zebrafish (Danio rerio) can be used in studies addressing the effects of drugs on learning, memory, and anxiety. In the present study, we investigated the effect of different alcohol treatments (chronic and acute) on the learning and anxiety response of zebrafish in an inhibitory avoidance paradigm. Zebrafish were initially exposed to different alcohol treatments and submitted to an inhibitory avoidance protocol, where an electroshock was applied to the fish as they swam from the white to the black side of a shuttle box tank (naturally preferred environment of zebrafish)...
July 17, 2017: Zebrafish
https://www.readbyqxmd.com/read/28714383/novel-mannich-bases-as-potential-anticonvulsants-syntheses-characterization-and-biological-evaluation
#2
Amit Kumar Keshari, Aseem Tewari, Shweta Singh Verma, Shailendra K Saraf
BACKGROUND: Mannich bases are known to be an important pharmacophore or bioactive leads in the synthesis of various potential agents that have a variety of therapeutic activities like anticancer, antipsychotic, anticonvulsant, antimalarial, anti-inflammatory, antibacterial and so forth. Thus, in the present research, conjugation of moieties like 1,5-benzoxazepines and 1,5-benzothiazepines with secondary amines like piperazine, methyl piperazine and morpholine was carried out in a Mannich base with an anticipation of good anticonvulsant activity...
July 17, 2017: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28707581/synthesis-and-evaluation-of-novel-diazaspiro-hydantoins-as-potential-anticonvulsants
#3
C S Ananda Kumar, B Veeresh, K C Ramesha, C S Ashok Raj, K M Mahadevaiah, S B Benaka Prasad
A series of novel diazaspiro compounds 6a-t were synthesised and biologically evaluated for their anticonvulsant activity in the maximal electroshock seizure (MES) assay. Most of the tested compounds exhibited moderate to weak activity in the MES screen test, The compounds 6f, 6h, 6i, 6j, 6p, 6s and 6n able to protect seizure effect significantly higher and this effect was similar when compared to standard drug treated rats.
July 12, 2017: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28702712/evaluation-of-the-anticonvulsant-effect-of-brilliant-blue-g-a-selective-p2x7-receptor-antagonist-in%C3%A2-the-iv-ptz-maximal-electroshock-and-6%C3%A2-hz-induced-seizure-tests-in-mice
#4
Dorota Nieoczym, Katarzyna Socała, Piotr Wlaź
Epilepsy is one of the most common neurological disorders which is diagnosed in around 65 million people worldwide. Clinically available antiepileptic drugs fail to control epileptic activity in about 30% of patients and they are merely symptomatic treatments and cannot cure or prevent epilepsy. There remains a need for searching new therapeutic strategies for epileptic disorders. The P2X7 receptor has been recently investigated as a new target in epilepsy treatment. Preclinical studies revealed that P2X7 receptor antagonists have anticonvulsant properties in some models of epilepsy...
July 12, 2017: Neurochemical Research
https://www.readbyqxmd.com/read/28686214/current-study-of-the-mechanism-of-action-of-the-potential-anti-epileptic-agent-q808
#5
Xiang Li, Hong-Jian Zhang, Qing Wang, Dian-Wen Zhang, Di Wu, Wei Li, Zhe-Shan Quan
Our previous study showed that the anticonvulsant Q808 might be effective against seizures induced by maximal electroshock, pentylenetetrazole (PTZ), isoniazid (ISO), thiosemicarbazide (THIO), and 3-mercaptopropionic acid (3-MP). In the present study, we explored the possible mechanism of action of Q808. Results obtained with high-performance liquid chromatography (HPLC) suggest that Q808 may affect neurotransmitter content in the brain, by specifically increasing GABA content in the rat hippocampus at doses of 40 mg/kg and 80 mg/kg, and by reducing the content of glutamate and glutamine in the rat thalamus at a dose of 80 mg/kg...
July 7, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28665338/molecular-docking-and-anticonvulsant-activity-of-newly-synthesized-quinazoline-derivatives
#6
Hatem A Abuelizz, Rabab El Dib, Mohamed Marzouk, El-Hassane Anouar, Yousreya A Maklad, Hanan N Attia, Rashad Al-Salahi
A new series of quinazoline-4(3H)-ones are evaluated for anticonvulsant activity. After intraperitoneal (ip) injection to albino mice at a dose of 100 mg/kg body weight, synthesized quinazolin-4(3H)-ones (1-24) were examined in the maximal electroshock (MES) induced seizures and subcutaneous pentylenetetrazole (scPTZ) induced seizure models in mice. The Rotarod method was applied to determine the neurotoxicity. Most of the compounds displayed anticonvulsant activity in the scPTZ screen at a dose range of 0...
June 30, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28635024/a-small-molecule-activator-of-nav-1-1-channels-increases-fast-spiking-interneuron-excitability-and-gabaergic-transmission-in-vitro-and-has-anti-convulsive-effects-in-vivo
#7
Kristen Frederiksen, Lu Dunguo, Jinhui Yang, Henrik Sindal Jensen, Jesper Frank Bastlund, Peter Hjørringgaard Larsen, Liu Henry, Kim Dekermendjian, Lassina Badolo, Morten Laursen, Charlotte Hougaard, Charles Yang, Niels Svenstrup, Morten Grunnet
Nav 1.1 (SCN1A) channels primarily located in gamma-aminobutyric acid (GABA)ergic fast-spiking interneurons are pivotal for action potential generation and propagation in these neurons. Inappropriate function of fast-spiking interneurons, leading to disinhibition of pyramidal cells and network desynchronization, correlates with decreased cognitive capability. Further, reduced functionality of Nav 1.1 channels is linked to various diseases in the central nervous system. There is, at present, however no subtype selective pharmacological activators of Nav 1...
June 21, 2017: European Journal of Neuroscience
https://www.readbyqxmd.com/read/28585447/anticonvulsant-effects-of-aerial-parts-of-verbena-officinalis-extract-in-mice-involvement-of-benzodiazepine-and-opioid-receptors
#8
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/28551543/justicia-spicigera-schltdl-and-kaempferitrin-as-potential-anticonvulsant-natural-products
#9
Ma Eva González-Trujano, Fabiola Domínguez, Gimena Pérez-Ortega, Miguel Aguillón, David Martínez-Vargas, Salvador Almazán-Alvarado, Adrián Martínez
Justicia spicigera Schltdl. is a vegetal species traditionally used to control epilepsy, but scientific evidence is required to reinforce this activity. The aim of the study was to evaluate the anticonvulsant-like activity of J. spicigera aqueous extract (JsAE) and a bioactive compound. JsAE was assessed in a dose-response manner (30, 100 and 1000mg/kg, i.p.) using the pentylenetetrazol (PTZ)-induced seizures and maximal electroshock seizure (MES) test in mice in comparison to ethosuximide (ETX, reference drug 100mg/kg, i...
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
#10
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...
July 12, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28458102/ivabradine-attenuates-the-anticonvulsant-potency-of-lamotrigine-but-not-that-of-lacosamide-pregabalin-and-topiramate-in-the-tonic-clonic-seizure-model-in-mice
#11
Katarzyna M Sawicka, Katarzyna Załuska, Agnieszka Wawryniuk, Karolina Załuska-Patel, Michał Szczyrek, Bartłomiej Drop, Jadwiga Daniluk, Monika Szpringer, Dorota Żółkowska, Jarogniew J Łuszczki
Hyperpolarization-activated cyclic nucleotide-gated (HCN) channels are involved not only in synaptic transmission and neuronal excitability under physiological conditions, but also in seizure activity. To determine the influence of ivabradine (an HCN channel inhibitor) on the anticonvulsant potency of four novel antiepileptic drugs (AEDs: lacosamide, lamotrigine, pregabalin and topiramate) in the mouse maximal electroshock-induced seizure (MES) model. Adult male albino Swiss mice were challenged with maximal electroconvulsions (electric current of 25mA delivered via auricular electrodes)...
July 2017: Epilepsy Research
https://www.readbyqxmd.com/read/28445732/the-hect-family-ubiquitin-ligase-eel-1-regulates-neuronal-function-and-development
#12
Karla J Opperman, Ben Mulcahy, Andrew C Giles, Monica G Risley, Rayna L Birnbaum, Erik D Tulgren, Ken Dawson-Scully, Mei Zhen, Brock Grill
Genetic changes in the HECT ubiquitin ligase HUWE1 are associated with intellectual disability, but it remains unknown whether HUWE1 functions in post-mitotic neurons to affect circuit function. Using genetics, pharmacology, and electrophysiology, we show that EEL-1, the HUWE1 ortholog in C. elegans, preferentially regulates GABAergic presynaptic transmission. Decreasing or increasing EEL-1 function alters GABAergic transmission and the excitatory/inhibitory (E/I) balance in the worm motor circuit, which leads to impaired locomotion and increased sensitivity to electroshock...
April 25, 2017: Cell Reports
https://www.readbyqxmd.com/read/28435427/novel-4-thiazolidinone-derivatives-as-agonists-of-benzodiazepine-receptors-design-synthesis-and-pharmacological-evaluation
#13
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/28427019/transplantation-of-inhibitory-precursor-cells-from-medial-ganglionic-eminence-produces-distinct-responses-in-two-different-models-of-acute-seizure-induction
#14
Daisyléa de Souza Paiva, Simone Amaro Alves Romariz, Maria Fernanda Valente, Luiz Bruno Moraes, Luciene Covolan, Maria Elisa Calcagnotto, Beatriz Monteiro Longo
Medial ganglionic eminence (MGE) is one of the sources of inhibitory interneurons during development. Following transplantation in postnatal developing brain, MGE cells can increase local inhibition suggesting a possible protection to GABAergic dysfunction in brain disorders, such as epilepsy. Since it has been shown that MGE-derived cells harvested as neurospheres are able to suppress seizures, it might be important to investigate whether these protective effects would change in different seizure models. Here, we used pentylenetetrazole-(PTZ) and maximal electroshock (MES)-induced seizure models to test whether the transplantation of MGE cells would increase the threshold to trigger acute seizures...
May 2017: Epilepsy & Behavior: E&B
https://www.readbyqxmd.com/read/28412310/increased-seizure-susceptibility-and-other-toxicity-symptoms-following-acute-sulforaphane-treatment-in-mice
#15
Katarzyna Socała, Dorota Nieoczym, Edyta Kowalczuk-Vasilev, Elżbieta Wyska, Piotr Wlaź
Activation of Nrf2 with sulforaphane has recently gained attention as a new therapeutic approach in the treatment of many diseases, including epilepsy. As a plant-derived compound, sulforaphane is considered to be safe and well-tolerated. It is widely consumed, also by patients suffering from seizure and taking antiepileptic drugs, but no toxicity profile of sulforaphane exists. Since many natural remedies and dietary supplements may increase seizure risk and potentially interact with antiepileptic drugs, the aim of our study was to investigate the acute effects of sulforaphane on seizure thresholds and activity of some first- and second-generation antiepileptic drugs in mice...
July 1, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28399089/-the-topical-problems-of-the-application-of-the-taser-electroshock-devices
#16
REVIEW
I V Kondratova, K Yu Kulinkovich
The objective of the present study was the analysis of publications in the foreign medical literature concerning the problems of safety, clinical diagnostics, pathological morphology, and treatment of the patients subjected to the impact by various models of the TASER electroshock devices. The materials for this article were borrowed from the available Internet resources and libraries. The methods of scientific analysis were employed to follow up the dynamics of publication and to determine the number of publications on the issues of interest...
2017: Sudebno-meditsinskaia Ekspertiza
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
#17
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/28372935/synthesis-and-biological-activity-of-novel-tert-amylphenoxyalkyl-homo-piperidine-derivatives-as-histamine-h3r-ligands
#18
Kamil J Kuder, Dorota Łażewska, Maria Kaleta, Gniewomir Latacz, Tim Kottke, Agnieszka Olejarz, Tadeusz Karcz, Andrzej Fruziński, Katarzyna Szczepańska, Janina Karolak-Wojciechowska, Holger Stark, Katarzyna Kieć-Kononowicz
As a continuation of our search for novel histamine H3 receptor ligands a series of twenty new tert-amyl phenoxyalkylamine derivatives (2-21) was synthesized. Compounds of four to eight carbon atoms spacer alkyl chain were evaluated on their binding properties at human histamine H3 receptor (hH3R). The highest affinities were observed for pentyl derivatives 6-8 (Ki=8.8-23.4nM range) and among them piperidine derivative 6 with Ki=8.8nM. Structures 6, 7 were also classified as antagonists in cAMP accumulation assay (with EC50=157 and 164nM, respectively)...
May 15, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28317156/synthesis-and-anticonvulsant-properties-of-new-3-3-diphenyl-2-5-dioxo-pyrrolidin-1-yl-acetamides-and-3-3-diphenyl-propionamides
#19
Jolanta Obniska, Anna Rapacz, Sabina Rybka, Małgorzata Góra, Paweł Żmudzki, Krzysztof Kamiński
The focused library of new amides derived from 3,3-diphenyl-2,5-dioxo-pyrrolidin-1-yl-acetic acid (2a-t) and 3,3-diphenyl-propionic acid (3a-t) as potential anticonvulsant agents was synthesized. The final products were obtained in the amidation reaction of the given carboxylic acid (2, 3) with appropriate secondary amines in the presence of carbonyldiimidazole (CDI) as a coupling reagent. The initial anticonvulsant screening was performed in mice intraperitoneally (i.p.) using the "classical" maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) seizure models, whereas the acute neurological toxicity was determined applying the rotarod test...
April 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/28315465/early-preclinical-evaluation-of-dihydropyrimidin-thi-ones-as-potential-anticonvulsant-drug-candidates
#20
Mariana Matias, Gonçalo Campos, Samuel Silvestre, Amílcar Falcão, Gilberto Alves
Although significant advances are occurring in epilepsy research, about 30% of epileptic patients are still inadequately controlled by standard drug therapy. For this reason, it continues to be important to develop new chemical entities through which epilepsy could be effectively controlled. In this study, the anticonvulsant activity of forty-two dihydropyrimidin(thi)ones was explored and their efficacy was evaluated in rodents against the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole tests...
March 15, 2017: European Journal of Pharmaceutical Sciences
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