Read by QxMD icon Read


Mustafa Ceylan, Umit M Kocyigit, Necibe Canan Usta, Belma Gürbüzlü, Yusuf Temel, Saleh H Alwasel, İlhami Gülçin
Benzothiazepine compounds have a wide range of applications such as antibacterial, antidepressants, anticonvulsants, antihypertensives, antibiotics, antifungal, hypnotic, enzyme inhibitors, antitumor, anticancer and anti-HIV agents. In this study, the synthesis of novel tetralone-based benzothiazepine derivatives (1-16) and their in vitro antibacterial activity and human carbonic anhydrase isoenzymes I and II (hCA I and II) inhibitory effects were investigated. Both isoenzymes were purified by sepharose-4B-l-tyrosine-sulfanilamide affinity chromatography from fresh human red blood cells...
October 25, 2016: Journal of Biochemical and Molecular Toxicology
Piotr Tutka, Maria W Kondrat-Wróbel, Katarzyna Zaluska, Dorota Żółkowska, Magdalena Florek-Łuszczki, Jarogniew J Łuszczki
BACKGROUND: Cytisine (CYT) is a partial agonist of brain α4β2 nicotinic acetylcholine receptors widely used in Central/Eastern Europe for smoking cessation. OBJECTIVES: This study evaluated the effect of CYT on the ability of classical and novel antiepileptic drugs to prevent seizures evoked by the 6-Hz test, a model of psychomotor seizures in mice thought as a model of drug-resistant seizures. RESULTS: CYT administered intraperitoneally (i...
October 25, 2016: Psychopharmacology
Yasuko Noda, Toshiki Masumizu, Akitane Mori
Methylguanidine (MG) is a known nephrotoxin and neurotoxin, and an intracisternal injection of MG can induce convulsions in experimental animals. In this in vitro study, we examined the inhibitory effects of the antiepileptic agent zonisamide (ZNS) on hydroxyl radicals (•OH) generated from MG by using an electron spin resonance (ESR) technique. ZNS scavenged •OH generated from MG in a dose-dependent manner through direct scavenging during the auto-oxidation of MG. The rate constant of ZNS reacting with the •OH was at a near diffusion-controlled rate...
October 2016: Acta Medica Okayama
Violina Angelova, Valentin Karabeliov, Pavlina A Andreeva-Gateva, Jana Tchekalarova
Preclinical Research Epilepsy is a chronic devastating neurological disorder characterized by synchronous interictal discharges. Treatment with antiepileptic drugs (AEDs) can alleviate spontaneous seizure activity without preventing the progression and development of epileptogenesis. Current design and development of new AEDs and strategies for the prevention of epilepsy is focused mainly on attenuating uncontrolled seizures, severe side effects and toxicity in chronic drug therapy. It has thus become necessary to discover new chemical pharmacophores with a broad spectrum of activity and less neurotoxicity...
October 24, 2016: Drug Development Research
Trond Myhrer, Pål Aas
The threat of chemical warfare agents like nerve agents requires life saving measures of medical pretreatment combined with treatment after exposure. Pretreatment (pyridostigmine) may cause some side effects in a small number of individuals. A comprehensive research on animals has been performed to clarify effects on behavior. The results from these studies are far from unambiguous, since pyridostigmine may produce adverse effects on behavior in animals in relatively high doses, but not in a consistent way...
October 20, 2016: Neuroscience and Biobehavioral Reviews
Kinga Sałat, Adrian Podkowa, Natalia Malikowska, Felix Kern, Jörg Pabel, Ewelina Wojcieszak, Katarzyna Kulig, Klaus T Wanner, Beata Strach, Elżbieta Wyska
BACKGROUND AND PURPOSE: Since GABAergic dysfunction underlies a variety of neurological and psychiatric disorders, numerous strategies leading to the augmentation of GABAergic neurotransmission have been introduced. One of them is the inhibition of GABA reuptake from the synaptic cleft mediated by four plasma membrane GABA transporters (GAT1-4). GAT1 which is exclusively expressed in the brain is an interesting target for centrally acting drugs. In this research, pharmacological properties of a novel, highly potent and selective inhibitor of GAT1, the guvacine derivative named DDPM-2571, were assessed in vivo...
October 19, 2016: Neuropharmacology
Simone A A Romariz, Daisyléa S Paiva, Layla T Galindo, Gabriela F Barnabé, Vivian A Guedes, Cesario V Borlongan, Beatriz M Longo
AIMS: Medial ganglionic eminence (MGE) progenitors give rise to inhibitory interneurons and may serve as an alternative cell source for large-scale cell transplantation for epilepsy after in vitro expansion. We investigated whether modifications in the culture medium of MGE neurospheres affect neuronal differentiation and expression of MGE-specific genes. In vivo, we compared anticonvulsant effects and cell differentiation pattern among neurospheres grown in different culture media and compared them with freshly harvested MGE cells...
October 21, 2016: CNS Neuroscience & Therapeutics
Nicole A Hawkins, Nicole J Zachwieja, Alison R Miller, Lyndsey L Anderson, Jennifer A Kearney
A substantial number of mutations have been identified in voltage-gated sodium channel genes that result in various forms of human epilepsy. SCN1A mutations result in a spectrum of severity ranging from mild febrile seizures to Dravet syndrome, an infant-onset epileptic encephalopathy. Dravet syndrome patients experience multiple seizures types that are often refractory to treatment, developmental delays, and elevated risk for SUDEP. The same sodium channel mutation can produce epilepsy phenotypes of varying clinical severity...
October 2016: PLoS Genetics
Mariana Matias, Samuel Silvestre, Amílcar Falcão, Gilberto Alves
BACKGROUND: Gastrodia elata Blume (G. elata) is a traditional Chinese herb used for centuries in folk medicine. Due to the claimed anticonvulsant properties of G. elata, it is expected that this herb continues to be a target of research, aiming to deepen the available knowledge on its biological activity and safety. PURPOSE: The current review aims to discuss the most recent advances on the elucidation of the phytochemical composition and anticonvulsant potential of G...
November 15, 2016: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
Mohammad Zarei, Arvin Najafi, Pejman Mansouri, Sadaf Sadeghi-Yazdankhah, Houshang Saberi, Mehran Moradi, Mahmoud Farzan
OBJECTIVES: Despite the progress in understanding acute pain physiology during recent decade, eighty percent of patients still suffer from post-operative discomfort. Pregabalin is an anticonvulsant agent that is approved for painful neuropathies in diabetic patients and post herpetic neuralgia. The main objective of the present study was to compare the improvement in post-operative pain management and patient lifestyle in 3 groups, as first group received placebo, second who received Pregabalin for one day and the last group those who received it for 14 days...
October 17, 2016: Clinical Neurology and Neurosurgery
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
Pasquale Striano, Vincenzo Belcastro, Antonietta Coppola, Carlo Minetti, Salvatore Striano
INTRODUCTION: Despite optimal medical treatment, up to 30% of patients with epilepsy continue to experience recurrent seizures, and the challenge for new more efficacious and better-tolerated drugs is continuing. New antiepileptic drugs include the evolution of preexisting drugs and new compounds identified through the investigation of additional molecular targets, such as SV2A synaptic vesicle protein, voltage-gated potassium channels, ionotropic and metabotropic glutamate receptors, and gap junctions...
October 5, 2016: Clinical Neuropharmacology
Vincenzo De Iuliis, Raimondo Gelormini, Mariarosaria Flacco, Giuseppe Moriello, Marika Caruso, Eugenia Barone, Maria Golato, Elena Toniato, Pio Conti, Stefano Martinotti
BACKGROUND: Valproate is a broad-spectrum anticonvulsant that is effective in the treatment of tonic-clonic, myoclonic and absence seizures as well as in partial seizures as a second-line drug. It has been widely demonstrated in the literature that the effect of valproate on type-A γ-aminobutyric acid (GABA-A) receptors may reduce relapse to ethanol abuse. This retrospective study evaluated a 3-year period in which 42 patients from the Department of Alcoholism and Substance Abuse (DASA) were treated with valproate...
March 2016: Drugs—Real World Outcomes
Andrew J Wyman, Bruce N Mayes, Jackeline Hernandez-Nino, Nigel Rozario, Sandra K Beverly, Andrew W Asimos
STUDY OBJECTIVE: Seizures account for 1.2% of all emergency department (ED) visits, with 24% of those representing first-time seizures. Our primary goal is to determine whether obtaining an electroencephalogram (EEG) in the ED after a first-time seizure can identify individuals appropriate for initiation of anticonvulsant therapy on ED discharge. Our secondary goals are to determine the association of historical and clinical seizure features with epileptic EEGs and to determine the interobserver agreement for the EEG interpretation...
October 10, 2016: Annals of Emergency Medicine
Sudipta Saha, Vinit Raj, Amit Rai
The chemistry of heterocyclic containing, 1,3,4-thiadiazole has been an interesting field of study from ancient years. Subsequently, 1,3,4-thiadiazole nucleus constitutes a significant class of compounds for new drug development. Recently, various 1,3,4-thiadiazole derivatives have been synthesized and evaluated their biological activities including antimicrobial, antituberculosis, antioxidant, anti-inflammatory, anticonvulsants, antidepressant and anxiolytic, antihypertensive, anticancer and antifungal activity...
October 13, 2016: Anti-cancer Agents in Medicinal Chemistry
Rimpi Arora, Rahul Deshmukh
Embelin, the main active constituent of Embelia ribes, has been reported to possess various pharmacological actions, including anti-inflammatory, antioxidant, anticonvulsant, and neuroprotective. The present study was designed to investigate neuroprotective mechanisms and therapeutic potential of embelin against intracerebroventricular streptozotocin (ICV-STZ)-induced experimental sporadic dementia in rats. STZ was infused bilaterally at the dose of (3 mg/kg/1 μl/1 min) ICV on day first and third. Spatial and non-spatial memory was evaluated using Morris water maze and object recognition task in rats...
October 15, 2016: Molecular Neurobiology
Hui Shao, Yang Yang, Ai-Ping Qi, Pian Hong, Guang-Xi Zhu, Xin-Yu Cao, Wei-Gang Ji, Zhi-Ru Zhu
Temporal lobe epilepsy (TLE) is one of the most refractory types of adult epilepsy, and treatment options remain unsatisfactory. Gastrodin (GAS), a phenolic glucoside used in Chinese herbal medicine and derived from Gastrodia elata Blume, has been shown to have remarkable anticonvulsant effects on various models of epilepsy in vivo. However, the mechanisms of GAS as an anticonvulsant drug remain to be established. By utilizing a combination of behavioral surveys, immunofluorescence and electrophysiological recordings, the present study characterized the anticonvulsant effect of GAS in a pilocarpine-induced status epilepticus (SE) rat model of TLE and explored the underlying cellular mechanisms...
October 14, 2016: Neurochemical Research
Sahar Moghbelinejad, Safar Alizadeh, Ghazaleh Mohammadi, Fatemeh Khodabandehloo, Zahra Rashvand, Reza Najafipour, Marjan Nassiri-Asl
The flavonoid quercetin has recently been reported to have neuroprotective effects, and the role of the gamma-aminobutyric acid A alpha 5 subunit (GABAA α5) receptor has been determined in some nervous system disorders. The aim of this study was to identify the molecular mechanism of the effect of quercetin administered at anticonvulsive doses on the expression of the GABAA α5 receptor gene in kainic acid (KA)-induced seizures in mice. The experimental animals were divided into four groups: control, KA, and KA + quercetin at 50 or 100 mg/kg, respectively...
October 14, 2016: Journal of Physiological Sciences: JPS
Sophie Gohy, Antoine Froidure, Patrick Lebecque
Drug reaction with eosinophilia and systemic symptom (DRESS) syndrome is a rare and severe side-effect, mainly described after intake of anticonvulsants, allopurinol, or antibiotics. It usually begins within 2 months after drug introduction. Symptoms include cutaneous rash, hematologic abnormalities, and internal organ involvement and the diagnosis might be challenging. This case report illustrates for the first time this life-threatening complication in a patient with cystic fibrosis (CF). In this case, withdrawal of the offending drug was sufficient for full recovery...
October 14, 2016: Pediatric Pulmonology
Melissa L Barker-Haliski, Taylor D Heck, E Jill Dahle, Fabiola Vanegas, Timothy H Pruess, Karen S Wilcox, H Steve White
OBJECTIVE: Infection with Theiler's murine encephalomyelitis virus (TMEV) in C57Bl/6J mice induces acute seizures and development of spontaneous recurrent seizures and behavioral comorbidities weeks later. The present studies sought to determine whether acute therapeutic intervention with an anti-inflammatory-based approach could prevent or modify development of TMEV-induced long-term behavioral comorbidities. Valproic acid (VPA), in addition to its prototypical anticonvulsant properties, inhibits histone deacetylase (HDAC) activity, which may alter expression of the inflammasome...
October 14, 2016: Epilepsia
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"