Read by QxMD icon Read


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
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
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
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
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
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
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
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
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
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
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
Amir Rashidian, Forogh Farhang, Habib Vahedi, Ahmad Reza Dehpour, Shahram Ejtemai Mehr, Saeed Mehrzadi, Seyed Mahdi Rezayat
BACKGROUND: Lippia citriodora Kunth is one of the Iranian traditional medicines for the treatment of convulsive disorders. The goal of this study is to investigate the anticonvulsant activity of the plant's leave ethanolic extract against electro- and chemoconvulsant-induced seizures in mice. METHODS: The anticonvulsant activity of the extract (200, 400, 800 mg/kg, per os, p.o.) was investigated in pentylenetetrazole (PTZ) and maximal electroshock (MES)-induced seizures in mice...
2016: International Journal of Preventive Medicine
Ming-Xia Song, Xianqing Deng, Bao-Qi Rao, Bin-Bin Cheng, Yi Wu, Hong Zeng, You-Gen Luo
A series of 2-substituted-6-(4H-1,2,4-triazol-4-yl)benzo[d]oxazoles (5a-p) were designed and synthesized. Their anticonvulsant activities were evaluated using maximal electroshock shock (MES) and subcutaneous pentylenetetrazole (scPTZ) seizure models in mice. Their antidepressant activities were screened with the forced swimming test (FST). All the compounds showed anti-MES activities in different degrees. Among which, 5g and 5j were the most promising compounds with ED50 values of 31.7 and 12.7 mg/kg, respectively...
August 22, 2016: CNS & Neurological Disorders Drug Targets
G S Taiwe, F C O Moto, S Pale, A K Kandeda, Amadou Dawe, N Kouemou, E R M Ayissi, G T Ngoupaye, J S K Njapdounke, G C N Nkantchoua, J P O Omam, D Pahaye, E Ngo Bum
Extracts of Feretia apodanthera Del. (Rubiaceae) have been extensively used in traditional Cameroonian medicine to treat a variety of diseases, including some neurological disorders. The present study was aimed to tests the anticonvulsant properties of the aqueous extract and the alkaloid fraction of the stem barks of Feretia apodanthera. The anticonvulsant investigation was carried out against bicuculline-, picrotoxin-, pentylenetetrazol-, Methyl-β-carboline-3-carboxylate-, N-Methyl-D-aspartate-, 4-aminopyridine-, and maximal electroshock-induced seizures or turning behavior in mice...
August 12, 2016: Epilepsy Research
Anna M Waszkielewicz, Karolina Słoczyńska, Elżbieta Pękala, Paweł Żmudzki, Agata Siwek, Anna Gryboś, Henryk Marona
A series of new xanthone derivatives have been synthesized and evaluated for their anticonvulsant properties in the maximal electroshock (MES), subcutaneous metrazole (ScMet) tests as well as for neurotoxicity in the rotarod (TOX) in mice, i.p. and rats, p.o. Compound 9: R,S-2-{2-[(1-hydroxybutan-2-yl]amino)ethoxy}-9H-xanthen-9-one and compound 12: R,S-2-{3-[(1-hydroxybutan-2-yl)amino]propoxy}-9H-xanthen-9-one exerted activity in rats, p.o. 2 and 4 h after administration, respectively. Therefore, metabolic stability of the compounds was evaluated with use of rats microsomes, resulting in half-life t1/2 136 and 108 min, respectively, indicating that either the metabolites are very active, or the parent compounds exert other ADME properties other than metabolism which influence the late onset of activity...
August 20, 2016: Chemical Biology & Drug Design
Wolfgang Löscher
Epilepsy, a prevalent neurological disease characterized by spontaneous recurrent seizures (SRS), is often refractory to treatment with anti-seizure drugs (ASDs), so that more effective ASDs are urgently needed. For this purpose, it would be important to develop, validate, and implement new animal models of pharmacoresistant epilepsy into drug discovery. Several chronic animal models with difficult-to-treat SRS do exist; however, most of these models are not suited for drug screening, because drug testing on SRS necessitates laborious video-EEG seizure monitoring...
August 8, 2016: Neurochemical Research
Hafiz Mawasi, David Bibi, Meir Bialer
A novel series of carbamoyl derivatives of alkylimidazole has been designed and their anticonvulsant activity was comparatively evaluated in the mice- and rats-maximal-electroshock (MES), subcutaneous-metrazol (scMet) seizure tests and the mice-6Hz psychomotor (6Hz) models. The ten new designed molecules contain in their chemical structure imidazole, alkyl side-chain and carbamate as three potential active moieties. In spite of the close structural features of the carbamoyl imidazole derivatives only compounds 7, 8, 13 and 16 were active at the MES test with ED50 values ranging from 12 to 20mg/kg coupled with high protective index (PI=TD50/ED50) values of 4...
September 15, 2016: Bioorganic & Medicinal Chemistry
Melissa L Barker-Haliski, Fabiola Vanegas, Matthew J Mau, Tristan K Underwood, H Steve White
OBJECTIVE: Some antiseizure drugs (ASDs) are associated with cognitive liability in patients with epilepsy, thus ASDs without this risk would be preferred. Little comparative pharmacology exists with ASDs in preclinical models of cognition. Few pharmacologic studies exist on the acute effects in rodents with chronic seizures. Predicting risk for cognitive impact with preclinical models may supply valuable ASD differentiation data. METHODS: ASDs (phenytoin [PHT]; carbamazepine [CBZ]; valproic acid [VPA]; lamotrigine [LTG]; phenobarbital [PB]; tiagabine [TGB]; retigabine [RTG]; topiramate [TPM]; and levetiracetam [LEV]) were administered equivalent to maximal electroshock median effective dose ([ED50]; mice, rats), or median dose necessary to elicit minimal motor impairment (median toxic dose [TD50]; rats)...
September 2016: Epilepsia
Farzaneh Zolfagharian, Bibi Marjan Razavi, Hossein Hosseinzadeh
OBJECTIVE: Regarding the anticonvulsant effects of Satureja hortensis (S . hortensis) in Avicenna's book: canon of medicine; the present study was undertaken to evaluate the anti- eplileptic effects of S . hortensis aqueous and ethanolic aerial part extracts. Furthermore, the mechanisms of their anticonvulsant activities were also evaluated. MATERIALS AND METHODS: Seizure was induced by Pentylentetrazol (PTZ) and MES (maximal electroshock) models. Mice were randomly divided into 8 groups; negative control (normal saline, 10ml/Kg), positive control (diazepam, 2 mg/kg), S...
May 2016: Avicenna Journal of Phytomedicine
R Ataee, A Falahati, M A Ebrahimzadeh, M Shokrzadeh
OBJECTIVE: Sambucus (S) spp. is reported to possess a variety of activities and has been used in traditional medicine for many years. In spite of CNS activity of this genus, nothing is known about the anticonvulsant activity of S. nigra. MATERIALS AND METHODS: Anticonvulsant activities of methanolic extracts of bark, fruit and leaf of S. nigra at doses of 250, 500 and 1000 mg kg-1 were determined by pentylenetetrazole (PTZ) induced and maximal electroshock (MES) induced convulsions in mice...
July 2016: European Review for Medical and Pharmacological Sciences
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"