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https://www.readbyqxmd.com/read/27932863/non-imidazole-based-histamine-h3-receptor-antagonists-with-anticonvulsant-activity-in-different-seizure-models-in-male-adult-rats
#1
Bassem Sadek, Ali Saad, Gniewomir Latacz, Kamil Kuder, Agnieszka Olejarz, Tadeusz Karcz, Holger Stark, Katarzyna Kieć-Kononowicz
A series of twelve novel non-imidazole-based ligands (3-14) was developed and evaluated for its in vitro binding properties at the human histamine H3 receptor (hH3R). The novel ligands were investigated for their in vivo protective effects in different seizure models in male adult rats. Among the H3R ligands (3-14) tested, ligand 14 showed significant and dose-dependent reduction in the duration of tonic hind limb extension in maximal electroshock (MES)-induced seizure model subsequent to acute systemic administration (5, 10, and 20 mg/kg, intraperitoneally), whereas ligands 4, 6, and 7 without appreciable protection in MES model were most promising in pentylenetetrazole (PTZ) model...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27916842/synthesis-and-pharmacological-evaluation-of-new-3-4-dihydroisoquinolin-derivatives-containing-heterocycle-as-potential-anticonvulsant-agents
#2
Hong-Jian Zhang, Qing-Kun Shen, Chun-Mei Jin, Zhe-Shan Quan
Two novel series of 3,4-dihydroisoquinolin with heterocycle derivatives (4a-t and 9a-e) were synthesized and evaluated for their anticonvulsant activity using maximal electroshock (MES) test and pentylenetetrazole (PTZ)-induced seizure test. All compounds were characterized by IR, ¹H-NMR, (13)C-NMR, and mass spectral data. Among them, 9-(exyloxy)-5,6-dihydro-[1,2,4]triazolo[3,4-a]isoquinolin-3(2H)-one (9a) showed significant anticonvulsant activity in MES tests with an ED50 value of 63.31 mg/kg and it showed wide margins of safety with protective index (PI > 7...
November 29, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/27915183/search-for-new-potential-anticonvulsants-with-anxiolytic-and-antidepressant-properties-among-derivatives-of-4-4-diphenylpyrrolidin-2-one
#3
Katarzyna Malawska, Aleksandra Rak, Beata Gryzło, Kinga Sałat, Małgorzata Michałowska, Elżbieta Żmudzka, Krzysztof Lodarski, Barbara Malawska, Katarzyna Kulig
BACKGROUND: The aim of this study was to synthesize a series of new N-Mannich bases derived from 4,4-diphenylpyrrolidin-2-one having differently substituted 4-phenylpiperazines as potential anticonvulsant agents with additional (beneficial) pharmacological properties. METHODS: The target compounds 8-12 were prepared in one step from the 4-substituted phenylpiperazines, paraformaldehyde, and synthesized 4,4-diphenylpyrrolodin-2-one (7) by a Mannich-type reaction...
September 22, 2016: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/27876250/structure-anticonvulsant-activity-studies-in-the-group-of-e-n-cinnamoyl-aminoalkanols-derivatives-monosubstituted-in-phenyl-ring-with-4-cl-4-ch3-or-2-ch3
#4
Agnieszka Gunia-Krzyżak, Dorota Żelaszczyk, Anna Rapacz, Ewa Żesławska, Anna M Waszkielewicz, Katarzyna Pańczyk, Karolina Słoczyńska, Elżbieta Pękala, Wojciech Nitek, Barbara Filipek, Henryk Marona
A series of twenty two (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH3 or 2-CH3 was designed, synthesized and evaluated for anticonvulsant activity in rodent models of seizures: maximal electroshock (MES) test, subcutaneous pentylenetetrazole (scPTZ) test, and 6-Hz test. There were identified three most active compounds: S-(2E)-N-(1-hydroxypropan-2-yl)-3-(2-methylphenyl)prop-2-enamide (5) (ED50 MES=42.56, ED50 scPTZ=58.38, ED50 6-Hz 44mA=42.27mg/kg tested in mice after intraperitoneal (i...
November 11, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27863026/design-and-synthesis-of-selurampanel-a-novel-orally-active-and-competitive-ampa-receptor-antagonist
#5
David Orain, Engin Tasdelen, Samuel Haessig, Manuel Koller, Anne Picard, Celine Dubois, Kurt Lingenhoehl, Sandrine Desrayaud, Phillip Floersheim, David Carcache, Stephan Urwyler, Joerg Kallen, Henri Mattes
A series of potent quinazolinedione sulfonamide antagonists of the α-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) receptor were designed and synthesized. The structure-activity relationships (SAR) and in vivo activity of the series were investigated. In particular, compound 1 S (selurampanel; N-[7-isopropyl-6-(2-methylpyrazol-3-yl)-2,4-dioxo-1H-quinazolin-3-yl]methanesulfonamide) has shown excellent oral potency against maximal electroshock seizure (MES)-induced generalized tonic-clonic seizures in rodents as well as significant activity in patients suffering from various forms of epilepsy...
November 15, 2016: ChemMedChem
https://www.readbyqxmd.com/read/27853355/anticonvulsant-effects-of-isomeric-nonimidazole-histamine-h3-receptor-antagonists
#6
Bassem Sadek, Ali Saad, Johannes Stephan Schwed, Lilia Weizel, Miriam Walter, Holger Stark
Phenytoin (PHT), valproic acid, and modern antiepileptic drugs (AEDs), eg, remacemide, loreclezole, and safinamide, are only effective within a maximum of 70%-80% of epileptic patients, and in many cases the clinical use of AEDs is restricted by their side effects. Therefore, a continuous need remains to discover innovative chemical entities for the development of active and safer AEDs. Ligands targeting central histamine H3 receptors (H3Rs) for epilepsy might be a promising therapeutic approach. To determine the potential of H3Rs ligands as new AEDs, we recently reported that no anticonvulsant effects were observed for the (S)-2-(4-(3-(piperidin-1-yl)propoxy)benzylamino)propanamide (1)...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27809820/effect-of-root-extracts-of-ficus-benghalensis-banyan-in-memory-anxiety-muscle-co-ordination-and-seizure-in-animal-models
#7
Dipesh Raj Panday, G P Rauniar
BACKGROUND: Ficus benghalensis L. (Banyan) is a commonly found tree in Eastern Nepal. Its different plant parts are used for various neurological ailments. This study was performed in mice to see its effects in various neuropharmacological parameters. METHODS: Passive-avoidance (memory), Open-field (anxiety), Pentobarbital-induced Sleep potentiation (sleep), Rota-rod (muscle-co-ordination), Pentylenetetrazol-Induced and Maximal Electroshock Seizure Tests were performed...
November 3, 2016: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/27799911/huperzine-a-provides-robust-and-sustained-protection-against-induced-seizures-in-scn1a-mutant-mice
#8
Jennifer C Wong, Stacey B B Dutton, Stephen D Collins, Steven Schachter, Andrew Escayg
De novo loss-of-function mutations in the voltage-gated sodium channel (VGSC) SCN1A (encoding Nav1.1) are the main cause of Dravet syndrome (DS), a catastrophic early-life encephalopathy associated with prolonged and recurrent early-life febrile seizures (FSs), refractory afebrile epilepsy, cognitive and behavioral deficits, and a 15-20% mortality rate. SCN1A mutations also lead to genetic epilepsy with febrile seizures plus (GEFS+), which is an inherited disorder characterized by early-life FSs and the development of a range of adult epilepsy subtypes...
2016: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/27780482/bitemporal-v-high-dose-right-unilateral-electroconvulsive-therapy-for-depression-a-systematic-review-and-meta-analysis-of-randomized-controlled-trials
#9
E Kolshus, A Jelovac, D M McLoughlin
BACKGROUND: Brief-pulse electroconvulsive therapy (ECT) is the most acutely effective treatment for severe depression though concerns persist about cognitive side-effects. While bitemporal electrode placement is the most commonly used form worldwide, right unilateral ECT causes less cognitive side-effects though historically it has been deemed less effective. Several randomized trials have now compared high-dose (>5× seizure threshold) unilateral ECT with moderate-dose (1.0-2.5× seizure threshold) bitemporal ECT to investigate if it is as effective as bitemporal ECT but still has less cognitive side-effects...
October 26, 2016: Psychological Medicine
https://www.readbyqxmd.com/read/27757273/evaluation-of-anti-epileptic-activity-of-leaf-extracts-of-punica-granatum-on-experimental-models-of-epilepsy-in-mice
#10
Gollapalle L Viswanatha, Marikunte V Venkataranganna, Nunna Bheema Lingeswara Prasad, Godavarthi Ashok
OBJECTIVES: This study was aimed to examine the anti-epileptic activity of leaf extracts of Punica granatum in experimental models of epilepsy in Swiss albino mice. MATERIALS AND METHODS: Petroleum ether leaf extract of P. granatum (PLPG), methanolic LPG (MLPG), and aqueous LPG (ALPG) extracts of P. granatum leaves was initially evaluated against 6-Hz-induced seizure model; the potent extract was further evaluated against maximal electroshock (MES) and pentylenetetrazole (PTZ)-induced convulsions...
September 2016: Journal of Intercultural Ethnopharmacology
https://www.readbyqxmd.com/read/27702668/influence-of-xanthotoxin-8-methoxypsoralen-on-the-anticonvulsant-activity-of-various-novel-antiepileptic-drugs-against-maximal-electroshock-induced-seizures-in-mice
#11
Mirosław Zagaja, Marta Andres-Mach, Paweł Patrzylas, Daniel Pyrka, Monika Szpringer, Magdalena Florek-Łuszczki, Dorota Żółkowska, Krystyna Skalicka-Woźniak, Jarogniew J Łuszczki
The aim of this study was to determine the effects of xanthotoxin (8-methoxypsoralen) on the protective action of 5 various second- and third-generation antiepileptic drugs (i.e., lacosamide, lamotrigine, oxcarbazepine, pregabalin and topiramate) in the mouse maximal electroshock-induced seizure model. Seizure activity was evoked in adult male albino Swiss mice by a current (25mA, 500V, 0.2s stimulus duration) delivered via auricular electrodes. Drug-related adverse effects were determined in the chimney, grip-strength and passive avoidance tests...
October 1, 2016: Fitoterapia
https://www.readbyqxmd.com/read/27697054/new-hybrid-anticonvulsants-based-on-the-pyrrolidine-2-5-dione-scaffold-with-broad-spectrum-of-activity-in-the-preclinical-studies
#12
Krzysztof Kamiński
The multifunctional ligands approach is one of the modern strategies in drug discovery especially in relation to diseases with complex pathomechanism, such as Alzheimer's disease, cancer, or epilepsy. According to this method different molecules with given biological properties are combined in a single chemical entity to provide complex and broad activity. Thus, with the aim of obtaining more efficacious antiepileptic drugs (AEDs) that will suppress different types of human seizures, the new hybrid anticonvulsants based on the pyrrolidine-2,5-dione scaffold have been described...
September 27, 2016: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/27680868/structural-exploration-of-quinazolin-4-3h-ones-as-anticonvulsants-rational-design-synthesis-pharmacological-evaluation-and-molecular-docking-studies
#13
Vinod G Ugale, Sanjay B Bari
Anticonvulsants effective against multiple seizures are of wide interest as antiepileptic drugs, especially if active against pharmaco-resistant seizures. Herein, we synthesized 16 different, rationally designed 2-((6,7-dimethoxy-4-oxo-2-phenylquinazolin-3(4H)-yl)amino)-N-(substituted phenyl)acetamides and screened for anticonvulsant activities through in vivo experiments. Compound 4d emerged as prototype with excellent anti-seizure action in mice against electroshock, chemically induced and pharmaco-resistant 6-Hz seizure models with no symptoms of neurotoxicity and hepatotoxicity (ED50  = 23...
September 28, 2016: Archiv der Pharmazie
https://www.readbyqxmd.com/read/27668426/modulating-behavior-in-c-elegans-using-electroshock-and-antiepileptic-drugs
#14
Monica G Risley, Stephanie P Kelly, Kailiang Jia, Brock Grill, Ken Dawson-Scully
The microscopic nematode Caenorhabditis elegans has emerged as a valuable model for understanding the molecular and cellular basis of neurological disorders. The worm offers important physiological similarities to mammalian models such as conserved neuron morphology, ion channels, and neurotransmitters. While a wide-array of behavioral assays are available in C. elegans, an assay for electroshock/electroconvulsion remains absent. Here, we have developed a quantitative behavioral method to assess the locomotor response following electric shock in C...
2016: PloS One
https://www.readbyqxmd.com/read/27644408/proconvulsant-effects-of-the-ketogenic-diet-in-electroshock-induced-seizures-in-mice
#15
Iwona Zarnowska, Jarogniew J Luszczki, Tomasz Zarnowski, Piotr Wlaz, Stanislaw J Czuczwar, Maciej Gasior
Among non-pharmacological treatments, the ketogenic diet (KD) has the strongest demonstrated evidence of clinical success in drug resistant epilepsy. In an attempt to model the anticonvulsant effects of the KD pre-clinically, the present study assessed the effects of the KD against electroshock-induced convulsions in mice. After confirming that exposure to the KD for 2 weeks resulted in stable ketosis and hypoglycemia, mice were exposed to electroshocks of various intensities to establish general seizure susceptibility...
September 20, 2016: Metabolic Brain Disease
https://www.readbyqxmd.com/read/27622736/antinociceptive-and-anticonvulsant-effects-of-the-monoterpene-linalool-oxide
#16
Flávia Negromonte Souto-Maior, Diogo Vilar da Fonsêca, Paula Regina Rodrigues Salgado, Lucas de Oliveira Monte, Damião Pergentino de Sousa, Reinaldo Nóbrega de Almeida
CONTEXT: Linalool oxide (OXL) (a monoterpene) is found in the essential oils of certain aromatic plants, or it is derived from linalool. The motivation for this work is the lack of psychopharmacological studies on this substance. OBJECTIVE: To evaluate OXL's acute toxicity, along with its anticonvulsant and antinociceptive activities in male Swiss mice. MATERIAL AND METHODS: OXL (50, 100 and 150 mg/kg, i.p.) was investigated for acute toxicity and in the Rota-rod test...
September 13, 2016: Pharmaceutical Biology
https://www.readbyqxmd.com/read/27613376/a-material-history-of-electroshock-therapy-electroshock-technology-in-europe-until-1945
#17
Lara Rzesnitzek, Sascha Lang
The article considers the history of electroshock therapy as a history of medical technology, professional cooperation and business competition. A variation of a history from below is intended; though not from the patients' perspective (Porter, Theory Soc 14:175-198, 1985), but with a focus on electrodes, circuitry and patents. Such a 'material history' of electroshock therapy reveals that the technical make-up of electroshock devices and what they were used for was relative to the changing interests of physicians, industrial companies and mental health politics; it makes an intriguing case for the Social Construction of Technology theory (Bijker et al...
September 9, 2016: NTM
https://www.readbyqxmd.com/read/27600732/resveratrol-lacks-protective-activity-against-acute-seizures-in-mouse-models
#18
Francesca Tomaciello, Karine Leclercq, Rafal M Kaminski
Resveratrol (3,4',5-stilbenetriol) is a natural product having diverse anti-inflammatory and antioxidant properties. The compound has a wide spectrum of pharmacological and metabolic activity, including cardioprotective, neuroprotective, anticarcinogenic and anti-aging effects reported in numerous studies. Some reports also suggest potential anticonvulsant properties of resveratrol. In the present study, we used in mice three different seizure models which are routinely applied in preclinical drug discovery...
October 6, 2016: Neuroscience Letters
https://www.readbyqxmd.com/read/27597416/new-arylalkyl-azole-derivatives-showing-anticonvulsant-effects-could-have-vgsc-and-or-gabaar-affinity-according-to-molecular-modeling-studies
#19
Suat Sari, Arzu Karakurt, Harun Uslu, F Betül Kaynak, Ünsal Çalış, Sevim Dalkara
(Arylalkyl)azoles (AAAs) emerged as a novel class of antiepileptic agents with the invention of nafimidone and denzimol. Several AAA derivatives with potent anticonvulsant activities have been reported so far, however neurotoxicity was usually an issue. We prepared a set of ester derivatives of 1-(2-naphthyl)-2-(1H-1,2,4-triazol-1-yl)ethanone oxime and evaluated their anticonvulsant and neurotoxic effects in mice. Most of our compounds were protective against maximal electroshock (MES)- and/or subcutaneous metrazol (s...
August 25, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27592363/in-silico-screening-and-evaluation-of-the-anticonvulsant-activity-of-docosahexaenoic-acid-like-molecules-in-experimental-models-of-seizures
#20
Ali Gharibi Loron, Soroush Sardari, Jamshid Narenjkar, Mohammad Sayyah
BACKGROUND: Resistance to antiepileptic drugs as well as intolerability in 20-30% of the patients raises demand for developing new drugs with improved efficacy and safety. Acceptable anticonvulsant activity, good tolerability, and inexpensiveness of docosahexaenoic acid (DHA), make it as a good candidate for designing and development of the new anticonvulsant medications. METHODS: Ten DHA-based molecules were screened based on in silico screening of DHA-like molecules by root-mean-square deviation of atomic positions, biological activity score of Professional Association for SQL Server and structural requirements suggested by pharmacophore design...
September 4, 2016: Iranian Biomedical Journal
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