keyword
MENU ▼
Read by QxMD icon Read
search

electroshock

keyword
https://www.readbyqxmd.com/read/28934547/multifunctional-hybrid-compounds-derived-from-2-2-5-dioxopyrrolidin-1-yl-3-methoxypropanamides-with-anticonvulsant-and-antinociceptive-properties
#1
Michał Abram, Mirosław Zagaja, Szczepan Mogilski, Marta Andres-Mach, Gniewomir Latacz, Sebastian Baś, Jarogniew J Łuszczki, Katarzyna Kieć-Kononowicz, Krzysztof Kamiński
The focused set of new pyrrolidine-2,5-diones as potential broad-spectrum hybrid anticonvulsants was described. These derivatives integrate on the common structural scaffold the chemical fragments of well-known antiepileptic drugs such as ethosuximide, levetiracetam, and lacosamide. Such hybrids demonstrated effectiveness in two of the most widely used animal seizure models, namely, the maximal electroshock (MES) test and the psychomotor 6 Hz (32 mA) seizure model. Compound 33 showed the highest anticonvulsant activity in these models (ED50 MES = 79...
September 21, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28926841/beneficial-combination-of-lacosamide-with-retigabine-in-experimental-animals-an-isobolographic-analysis
#2
Jarogniew J Luszczki, Mirosław Zagaja, Barbara Miziak, Maria W Kondrat-Wrobel, Katarzyna Zaluska, Paula Wroblewska-Luczka, Piotr Adamczuk, Stanislaw J Czuczwar, Magdalena Florek-Luszczki
BACKGROUND/AIM: To isobolographically determine the types of interactions that occur between retigabine and lacosamide (LCM; two third-generation antiepileptic drugs) with respect to their anticonvulsant activity and acute adverse effects (sedation) in the maximal electroshock-induced seizures (MES) and chimney test (motor performance) in adult male Swiss mice. METHODS: Type I isobolographic analysis for nonparallel dose-response effects for the combination of retigabine with LCM (at the fixed-ratio of 1:1) in both the MES and chimney test in mice was performed...
September 20, 2017: Pharmacology
https://www.readbyqxmd.com/read/28867572/pharmacokinetic-and-pharmacodynamic-interaction-of-hydroalcoholic-extract-of-ocimum-sanctum-with-valproate
#3
Sudhir Chandra Sarangi, Dipesh Joshi, Ritesh Kumar, Thomas Kaleekal, Yogendra Kumar Gupta
For effective control of seizures, antiepileptic drugs (AEDs) are administered at higher dose which is associated with several adverse effects. This study envisaged antiepileptic and neuroprotective potential of Tulsi, a commonly used herb for its immunomodulatory property. The optimal dose of Ocimum sanctum hydroalcoholic extract (OSHE) was determined using maximal electroshock seizure (MES)- and pentylenetetrazol (PTZ)-induced seizure models in Wistar rats (200-250g) after administering OSHE (200-1000mg/kg) orally for 14days...
August 31, 2017: Epilepsy & Behavior: E&B
https://www.readbyqxmd.com/read/28863231/design-synthesis-and-pharmacological-screening-of-pyridazinone-hybrids-as-anticonvulsant-agents
#4
Sangh Partap, Mohammad Shahar Yar, Md Zaheen Hassan, Md Jawaid Akhtar, Anees A Siddiqui
A series of new hybrid benzimidazole containing pyridazinones derivatives were designed and synthesized in accordance with the pharmacophoric requirements essential for the anticonvulsant activity. The synthesized compounds were evaluated for anticonvulsant activity on mice by the gold standard maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ)-induced seizure models. Among the compounds tested, SS-4F showed significant anticonvulsant activity in both the screens with ED50 values of 25.10 and 85...
September 1, 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/28839381/anti-epileptic-effects-of-valepotriate-isolated-from-valeriana-jatamansi-jones-and-its-possible-mechanisms
#5
An Wu, Xia Ye, Qiang Huang, Wei-Min Dai, Jian-Min Zhang
OBJECTIVE: This work aimed to investigate the anti-epileptic effects of valepotriate isolated from Valeriana jatamansi Jones and studied its possible mechanisms. METHODS: The anti-epileptic effects of valepotriate were studied using maximal electroshock-induced seizure (MES), pentylenetetrazole (PTZ)-induced epilepsy, and pentobarbital sodium-induced sleeping model in mice. The possible anti-epileptic mechanisms of valepotriate were investigated by analyzing the expressions of GABAA, GABAB, glutamic acid decarboxylase (GAD65), Bcl-2, and caspase-3 in the brain using Western blot assay...
July 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/28806600/design-synthesis-and-evaluation-of-newer-5-6-dihydropyrimidine-2-1h-thiones-as-gaba-at-inhibitors-for-anticonvulsant-potential
#6
Meeta Sahu, Nadeem Siddiqui, Ramsha Iqbal, Vidushi Sharma, Sharad Wakode
Several new 5,6-dihydropyrimidine-2(1H)-thione derivatives have been prepared and investigated for their potencies for anticonvulsant activity against maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) test in mice. The acute neurotoxicity was measured by rotarod test. Compounds 3c and 3l were found active in both of the animal models. Further, in vitro GABA-AT enzyme activity assay was carried out to investigate the possible mechanism of action through GABA-AT inhibition. The most potent compounds 3c and 3l showed inhibitory potency (IC50) of 18...
July 28, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28804613/novel-derivatives-of-phthalimide-with-potent-anticonvulsant-activity-in-ptz-and-mes-seizure-models
#7
Asghar Davood, Maryam Iman, Hanieh Pouriaiee, Hamed Shafaroodi, Sepideh Akhbari, Leila Azimidoost, Erfan Imani, Somaieh Rahmatpour
OBJECTIVES: Phthalimide-based derivatives have anticonvulsant activity like as phenytoin by inhibition of sodium channel. In our previously research we mentioned about some phthalimide derivatives as potent anticonvulsant agents. MATERIALS AND METHODS: Fourteen analogs of 2-substituted phthalimide pharmacophore were synthesized and then were evaluated for the anticonvulsant activities in pentylenetetrazole-induced seizures (PTZ) and maximal electroshock seizure (MES) models...
April 2017: Iranian Journal of Basic Medical Sciences
https://www.readbyqxmd.com/read/28794189/time-of-day-influences-on-respiratory-sequelae-following-maximal-electroshock-induced-seizures-in-mice
#8
Benton S Purnell, Michael A Hajek, Gordon F Buchanan
Sudden unexpected death in epilepsy (SUDEP) is the leading cause of death in refractory epilepsy patients. While specific mechanisms underlying SUDEP are not well understood, evidence suggests most SUDEP occurs due to seizure-induced respiratory arrest. SUDEP also tends to happen at night. While this may be due to circumstances humans find themselves in at night, such as being alone without supervision or sleeping prone, or due to independent influences of sleep state, there are a number of reasons why the night (i...
August 9, 2017: Journal of Neurophysiology
https://www.readbyqxmd.com/read/28758238/design-synthesis-and-docking-study-of-pyrimidine-triazine-hybrids-for-gaba-estimation-in-animal-epilepsy-models
#9
Meeta Sahu, Nadeem Siddiqui, Mohd Javed Naim, Ozair Alam, Mohammad Shahar Yar, Vidushi Sharma, Sharad Wakode
A series of new pyrimidine-triazine hybrids (4a-t) was designed and synthesized, from which potent anticonvulsant agents were identified. Most of the compounds exhibited promising anticonvulsant activity against the maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) tests, along with minimal motor impairment with higher safety compared to the standard drugs, phenytoin and carbamazepine. In the series, 5-(4-(4-fluorophenyl)-6-(4-hydroxyphenyl)-2-thioxo-5,6-dihydropyrimidin-1(2H)-yl)-1,2-dihydro-1,2,4-triazin-3(6H)-one (4o) and 5-(6-(4-hydroxy-3-methoxyphenyl)-4-(4-hydroxyphenyl)-2-thioxo-5,6-dihydropyrimidin-1(2H)-yl)-1,2-dihydro-1,2,4-triazin-3(6H)-one (4s) emerged as most potent anticonvulsant agents with median doses of 22...
July 31, 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/28729118/hbk-14-and-hbk-15-triple-5-ht1a-5-ht7-and-5-ht3-antagonists-with-potent-antidepressant-and-anxiolytic-like-properties-increase-seizure-threshold-in-various-seizure-tests-in-mice
#10
Karolina Pytka, Katarzyna Socała, Anna Rapacz, Dorota Nieoczym, Mateusz Pieróg, Anna Gryboś, Agata Siwek, Anna Waszkielewicz, Piotr Wlaź
Most antidepressants lower seizure threshold, which might be due to the modulation of serotonergic neurotransmission. Here, we investigated the effects of two 5-HT1A, 5-HT7 and 5-HT3 antagonists, i.e., 1-(2-(2-(2,6-dimethylphenoxy)ethoxy)ethyl)-4-(2-methoxyphenyl)piperazine hydrochloride (HBK-14) and 1-{2-[2-(2-chloro-6-methylphenoxy)ethoxy]ethyl}-4-(2-methoxyphenyl)piperazine hydrochloride (HBK-15), with antidepressant- and anxiolytic-like properties, on seizure thresholds in three acute seizure tests, i.e...
October 3, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/28714785/effects-of-alcohol-on-inhibitory-avoidance-learning-in-zebrafish-danio-rerio
#11
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
#12
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
#13
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
#14
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
#15
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
#16
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%C3%A2-vitro-and-has-anti-convulsive-effects-in%C3%A2-vivo
#17
Kristen Frederiksen, Dunguo Lu, Jinhui Yang, Henrik Sindal Jensen, Jesper Frank Bastlund, Peter Hjørringgaard Larsen, Henry Liu, François Crestey, 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...
August 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
#18
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
#19
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
#20
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
keyword
keyword
45636
1
2
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"