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https://www.readbyqxmd.com/read/28092111/design-and-synthesis-of-5-substituted-benzo-d-1-3-dioxole-derivatives-as-potent-anticonvulsant-agents
#1
Shiyang Dong, Tiantian Wang, Chundi Hu, Xiaodong Chen, Yi Jin, Zengtao Wang
A series of 5-substituted benzo[d][1,3]dioxole derivatives was designed, synthesized, and tested for anticonvulsant activity using the maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) screens. Neurotoxicity was determined by rotarod test. In the preliminary screening, six compounds, 3a, 3c, 3d, and 4d-f, showed promising anticonvulsant activities in the MES model, and compounds 4c and 4d exhibited full protection against seizures at doses of 300 mg/kg in the scPTZ model. Among the synthesized compounds, 3c as the most active compound showed high protection against the MES-induced seizures with an ED50 value of 9...
January 16, 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/28063720/a-case-of-cardiac-arrest-that-occurred-on-a-high-mountain-in-which-a-favorable-outcome-was-obtained
#2
Youichi Yanagawa, Kazuhiko Omori, Ikuto Takeuchi, Kei Jitsuiki, Toshihiko Yoshizawa, Kouhei Ishikawa, Yumi Kando, Mutsumu Fukata, Hiromichi Ohsaka
A 36-year-old man started to climb Mount Fuji (3776m above sea level: ASL), from the Gotemba new fifth station (2400m ASL). He had no significant medical history, and this was his first attempt to climb such a high mountain. He began feeling chest discomfort but continued to climb. When he reached the ninth station of the mountain (3600mASL), he lost consciousness. One individual immediately provided basic life support using an automated external defibrillator (AED) that was located in the station. After electroshocks, he regained consciousness...
October 24, 2016: American Journal of Emergency Medicine
https://www.readbyqxmd.com/read/28056730/synthesis-molecular-docking-and-evaluation-of-3-4-2-amino-4-substitutedphenyl-2h-1-3-oxazin-thiazin-6-yl-2-phenyl-3h-quinazolin-4-one-derivatives-for-their-anticonvulsant-activity
#3
Nimisha Jain, Jugnu Jaiswal, Ashish Pathak, Pradeep Kumar Singour
BACKGROUND: According to World Health Organization (WHO), around 50 million people worldwide suffering from epilepsy. Therefore, continued search for safer and more effective anticonvulsants is urgently necessary. OBJECTIVES: The present work was to synthesize 2-phenyl substituted quiazolinone derivatives and to evaluate them for anticonvulsant activity and neurotoxic. METHODS: A series of novel 3-{4-[2-amino-4-(substitutedphenyl)-2H-[1.3] oxazin/thiazin-6-yl} 2-phenyl-3H-quinazolin-4-one derivatives were synthesized and evaluated for their anticonvulsant activity...
January 4, 2017: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28040846/design-synthesis-and-evaluation-of-5-substituted-1-h-tetrazoles-as-potent-anticonvulsant-agents
#4
Ai-Mei Liao, Tiantian Wang, Bangrong Cai, Yi Jin, Seunghoon Cheon, ChangJu Chun, Zengtao Wang
A series of 5-substituted 1-H-tetrazoles were designed and synthesized as potent anticonvulsant agents. Their preliminary anticonvulsant activities were evaluated using maximal electroshock and subcutaneous pentylenetetrazole (scPTZ) seizure tests. Neurotoxicity was determined using rotarod test. The results indicated that the compound 2j in scPTZ model exhibited the ED50 values of 83.3 mg/kg, superior to the standard drug ethosuximide with the maximum activity. In addition, compound 2k showed the most potent activity in MES model with ED50 value of 9...
December 31, 2016: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28011703/optogenetic-termination-of-ventricular-arrhythmias-in-the-whole-heart-towards-biological-cardiac-rhythm-management
#5
Emile C A Nyns, Annemarie Kip, Cindy I Bart, Jaap J Plomp, Katja Zeppenfeld, Martin J Schalij, Antoine A F de Vries, Daniël A Pijnappels
AIMS: Current treatments of ventricular arrhythmias rely on modulation of cardiac electrical function through drugs, ablation or electroshocks, which are all non-biological and rather unspecific, irreversible or traumatizing interventions. Optogenetics, however, is a novel, biological technique allowing electrical modulation in a specific, reversible and trauma-free manner using light-gated ion channels. The aim of our study was to investigate optogenetic termination of ventricular arrhythmias in the whole heart...
December 23, 2016: European Heart Journal
https://www.readbyqxmd.com/read/28009436/pharmacological-characterisation-of-n-2s-5-6-fluoro-3-pyridinyl-2-3-dihydro-1h-inden-2-yl-2-propanesulfonamide-a-novel-clinical-ampa-receptor-positive-allosteric-modulator
#6
Simon E Ward, Paul Beswick, Novella Calcinaghi, Lee A Dawson, Jane Gartlon, Francesca Graziani, Declan N C Jones, Laurent Lacroix, M H Selina Mok, Beatrice Oliosi, Joanne Pardoe, Kathryn Starr, Marie L Woolley, Mark H Harries
BACKGROUND AND PURPOSE: AMPA receptor positive allosteric modulators represent a potential therapeutic strategy to improve cognition in people with schizophrenia. These studies collectively constitute the pre-clinical pharmacology data package used to build confidence in the pharmacology of this molecule and enable a clinical trial application. EXPERIMENTAL APPROACH: [N-[(2S)-5-(6-fluoro-3-pyridinyl)-2,3-dihydro 1H-inden-2-yl]-2-propanesulfonamide] (UoS12258) was profiled in a number of in vitro and in vivo studies to highlight its suitability as a novel therapeutic agent...
December 23, 2016: British Journal of Pharmacology
https://www.readbyqxmd.com/read/27998332/-electroshock-therapy-in-the-third-reich
#7
Lara Rzesnitzek, Sascha Lang
The history of 'electroshock therapy' (now known as electroconvulsive therapy (ECT)) in Europe in the Third Reich is still a neglected chapter in medical history. Since Thomas Szasz's 'From the Slaughterhouse to the Madhouse', prejudices have hindered a thorough historical analysis of the introduction and early application of electroshock therapy during the period of National Socialism and the Second World War. Contrary to the assumption of a 'dialectics of healing and killing', the introduction of electroshock therapy in the German Reich and occupied territories was neither especially swift nor radical...
January 2017: Medical History
https://www.readbyqxmd.com/read/27932863/non-imidazole-based-histamine-h3-receptor-antagonists-with-anticonvulsant-activity-in-different-seizure-models-in-male-adult-rats
#8
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
#9
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
#10
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...
February 2017: 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
#11
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...
January 15, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27863026/design-and-synthesis-of-selurampanel-a-novel-orally-active-and-competitive-ampa-receptor-antagonist
#12
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
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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...
December 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
#19
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
#20
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...
November 2016: Archiv der Pharmazie
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