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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/28088732/apelin-13-protects-rat-primary-cortical-glia-neuron-co-culture-against-pentylenetetrazole-induced-toxicity
#2
Taj Pari Kalantaripour, Saeed Esmaeili-Mahani, Vahid Sheibani, Hamid Najafipour, Majid Asadi-Shekaari M
In spite of recent advances in the treatment of epilepsy, up to 35% of people living with the condition do not respond to accessible anti-epileptic drugs (AEDs) and continue to experience regular, devastating and potentially life-threatening seizures. Neuronal death is a significant feature of epilepsy in humans and experimental models. It has been reported that apelin, an endogenous ligand for the angiotensin-1-like receptor (APJ), has anticonvulsive as well as protective effects in some neurodegenerative situations...
January 12, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28088383/evaluating-the-role-of-astrocytes-on-%C3%AE-estradiol-effect-on-seizures-of-pilocarpine-epileptic-model
#3
Masoumeh Sarfi, Mahmoud Elahdadi Salmani, Iran Goudarzi, Taghi Lashkar Boluki, Kataneh Abrari
Epilepsy with periodic and unpredictable seizures is associated with hippocampal glutamate toxicity and tissue reorganization. Astrocytes play an important role in mediating the neuroprotective effects of estradiol and reducing seizure severity. Accordingly, the protective effects of low and high doses of estradiol on behavioral, astrocytic involvement and neuronal survival aspects of Pilocarpine-induced epilepsy were investigated. Lithium- Pilocarpine (30mg/kg) model was used to provoke epilepsy. Βeta-estradiol (2,40μg/ µl) was injected subcutaneously from 48 before to 48h after seizure induction...
January 11, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28088231/efficacy-of-gabapentin-for-prevention-of-postherpetic-neuralgia-study-protocol-for-a-randomized-controlled-clinical-trial
#4
Manuel Rullán, Oana Bulilete, Alfonso Leiva, Aina Soler, Antonia Roca, María José González-Bals, Patricia Lorente, Joan Llobera
BACKGROUND: Postherpetic neuralgia (PHN) is a chronic neuropathic pain that results from alterations of the peripheral nervous system in areas affected by the herpes zoster virus. The symptoms include pain, paresthesia, dysesthesia, hyperalgesia, and allodynia. Despite the availability of pharmacological treatments to control these symptoms, no treatments are available to control the underlying pathophysiology responsible for this disabling condition. METHODS/DESIGN: Patients with herpes zoster who are at least 50 years old and have a pain score of 4 or higher on a visual analogue scale (VAS) will be recruited...
January 14, 2017: Trials
https://www.readbyqxmd.com/read/28087250/pharmacology-of-cannabinoids-in-the-treatment-of-epilepsy
#5
REVIEW
Tyler E Gaston, Daniel Friedman
The use of cannabis products in the treatment of epilepsy has long been of interest to researchers and clinicians alike; however, until recently very little published data were available to support its use. This article summarizes the available scientific data of pharmacology from human and animal studies on the major cannabinoids which have been of interest in the treatment of epilepsy, including ∆9-tetrahydrocannabinol (∆9-THC), cannabidiol (CBD), ∆9-tetrahydrocannabivarin (∆9-THCV), cannabidivarin (CBDV), and ∆9-tetrahydrocannabinolic acid (Δ9-THCA)...
January 10, 2017: Epilepsy & Behavior: E&B
https://www.readbyqxmd.com/read/28076878/sumatriptan-an-antimigraine-drug-inhibits-pentylenetetrazol-induced-seizures-in-nmri-mice
#6
Abolfazl Jand, Mohammad Palizvan
Sumatriptan has been used for the acute treatment of migraine attacks. There are many similarities between migraine and epilepsy and the medications used to treat one of these disorders can effectively be used to treat the other. The purpose of this study was to evaluate and compare the anticonvulsant effects of sumatriptan with sodium valproate in NMRI mice. 62 male NMRI mice were divided into 8 groups. The groups consisted of a saline (control) group, 4 intraperitoneally (ip) administered sumatriptan groups (1, 10, 50, and 100 mg/kg, ip), and 3 sodium valproate groups (50, 150, and 300 mg/kg, ip)...
January 11, 2017: Drug Research
https://www.readbyqxmd.com/read/28067623/seizure-control-through-genetic-and-pharmacological-manipulation-of-pumilio-a-key-component-of-neuronal-homeostasis
#7
Wei-Hsiang Lin, Carlo N G Giachello, Richard A Baines
Epilepsy is a significant disorder for which approximately one-third of patients do not respond to drug treatments. Next-generation drugs, which interact with novel targets, are required to provide a better clinical outcome for these individuals. To identify potential novel targets for antiepileptic drug (AED) design, we used RNA sequencing to identify changes in gene transcription in two seizure models of the fruitfly Drosophila melanogaster The first model compared gene transcription between wildtype (WT) and the bangsenseless(1) (para(bss)) mutant; a gain-of-function in the sole fly voltage-gated sodium channel (paralytic)...
December 14, 2016: Disease Models & Mechanisms
https://www.readbyqxmd.com/read/28066149/neuroprotective-effect-of-lithium-after-pilocarpine-induced-status-epilepticus-in-mice
#8
Namgue Hong, Yun-Sik Choi, Seong Yun Kim, Hee Jung Kim
Status epilepticus is the most common serious neurological condition triggered by abnormal electrical activity, leading to severe and widespread cell loss in the brain. Lithium has been one of the main drugs used for the treatment of bipolar disorder for decades, and its anticonvulsant and neuroprotective properties have been described in several neurological disease models. However, the therapeutic mechanisms underlying lithium's actions remain poorly understood. The muscarinic receptor agonist pilocarpine is used to induce status epilepticus, which is followed by hippocampal damage...
January 2017: Korean Journal of Physiology & Pharmacology
https://www.readbyqxmd.com/read/28065184/long-term-outcomes-in-the-management-of-painful-diabetic-neuropathy
#9
Lauren M Mai, A John Clark, Allan S Gordon, Mary E Lynch, Pat K Morley-Forster, Howard Nathan, Catherine Smyth, Larry W Stitt, Cory Toth, Mark A Ware, Dwight E Moulin
BACKGROUND: Painful diabetic neuropathy (PDN) is a frequent complication of diabetes mellitus. Current treatment recommendations are based on short-term trials, generally of ≤3 months' duration. Limited data are available on the long-term outcomes of this chronic disease. The objective of this study was to determine the long-term clinical effectiveness of the management of chronic PDN at tertiary pain centres. METHODS: From a prospective observational cohort study of patients with chronic neuropathic non-cancer pain recruited from seven Canadian tertiary pain centres, 60 patients diagnosed with PDN were identified for analysis...
January 9, 2017: Canadian Journal of Neurological Sciences. le Journal Canadien des Sciences Neurologiques
https://www.readbyqxmd.com/read/28064419/pharmacokinetics-and-pharmacogenetics-of-carbamazepine-in-children
#10
Natasa Djordjevic, Slobodan M Jankovic, Jasmina R Milovanovic
Although carbamazepine is one of the oldest anticonvulsant drugs, it is still heavily utilized for treatment of epilepsy in children. The aim of this article was to review the current knowledge about pharmacokinetics and pharmacogenetics of carbamazepine in children. The literature for this review was systematically searched for in the MEDLINE and SCINDEKS databases. Oral bioavailability of carbamazepine in children is about 75-85%, and it is approximately 75-85% bound to plasma proteins. Apparent volume of distribution is 1...
January 7, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28057897/review-and-update-of-the-hong-kong-epilepsy-guideline-on-status-epilepticus
#11
REVIEW
E Lw Fung, B Bh Fung
Convulsive status epilepticus is the most extreme form of seizure. It is a medical and neurological emergency that requires prompt and appropriate treatment. Treatment of convulsive status epilepticus is usually divided into stages/steps. The International League Against Epilepsy has released a new definition of status epilepticus that may help to unify the definition in future studies. Over the last few years new information has become available regarding its management. The Rapid Anticonvulsant Medication Prior to Arrival Trial demonstrated non-inferiority of intramuscular midazolam in early status epilepticus compared with intravenous lorazepam...
January 6, 2017: Hong Kong Medical Journal, Xianggang Yi Xue za Zhi
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
#12
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/28054742/evaluation-of-dna-damage-in-hepg2-cells-and-mutagenicity-of-garcinielliptone-fc-a-bioactive-benzophenone
#13
Lismare da Silva Prado, Juliana da Silva, Ana Letícia Hilario Garcia, Fernanda Brião Menezes Boaretto, Ivana Grivicich, Lucas Umpierre Conter, Aguisson de Oliveira Salvi, Flávio Henrique Reginatto, Suele Bierhals Vencato, Alexandre de Barros Falcão Ferraz, Jaqueline Nascimento Picada
Garcinielliptone FC (GFC) is a polyprenylated benzophenone isolated from the hexanic extract of Platonia insignis seeds with potential pharmacological effects on the central nervous system. In a pre-clinical study, this compound showed anticonvulsant action, becoming a candidate to treat epilepsy disorders. However, genotoxicological aspects of GFC should be known to ensure its safe use. This study investigated the cytotoxic, genotoxic and mutagenic effects of GFC. Cytotoxicity was evaluated using the colourimetric assay of MTT (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide) in human hepatoma cells (HepG2) (2 - 100 μg/mL) for 3, 6 and 24 hr...
January 5, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28043841/non-opioid-pain-management-in-benign-minimally-invasive-hysterectomy-a-systematic-review
#14
REVIEW
Emily Blanton, Georgine Lamvu, Insiyyah Patanwala, Kenneth I Barron, Kathryn Witzeman, Frank F Tu, Sawsan As-Sanie
BACKGROUND: Less postoperative pain is typically associated with a minimally invasive hysterectomy compared to a laparotomy approach but poor pain control can still be an issues. Multiple guidelines exist for managing postoperative pain yet most are not specialty-specific and are based on procedures bearing little relevance to a minimally invasive hysterectomy. OBJECTIVE: To determine if there is enough quality evidence within the benign gynecology literature to make non-opioid pain control recommendations for women undergoing a benign minimally invasive hysterectomy...
December 30, 2016: American Journal of Obstetrics and Gynecology
https://www.readbyqxmd.com/read/28040846/design-synthesis-and-evaluation-of-5-substituted-1-h-tetrazoles-as-potent-anticonvulsant-agents
#15
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/28039625/the-influence-of-maternal-exposure-history-to-virus-and-medicine-during-pregnancy-on-congenital-heart-defects-of-fetus
#16
Qianhong Liang, Wei Gong, Dongming Zheng, Risheng Zhong, Yunjie Wen, Xiaodan Wang
Congenital heart disease (CHD) is the most common birth defect. It is due to dysfunction of the heart and great vessels during embryo development stage, or the channel was not closed after birth. This study focuses on investigating the influence of virus infection and medicine history during pregnancy on the incidence rate of CHD of fetus. We conducted a retrospective birth cohort study of infant born in the maternal and child health hospital of Fanyu district in Guangzhou. Five thousand three hundred eighty one cases with complete medical records, including mothers, fathers, and infants, were enrolled...
December 30, 2016: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/28030918/to-treat-or-not-to-treat-drug-refractory-epilepsy-by-the-ketogenic-diet-that-is-the-question
#17
REVIEW
Marzena Ułamek-Kozioł, Ryszard Pluta, Anna Bogucka-Kocka, Stanisław J Czuczwar
Epilepsy is a serious neurologic disorder worldwide which affects about 1% of the population (ca. 50 million people), the highest prevalence occurring in both children and elderly. Apart from idiopathic forms, etiology of the disease involves multiple brain risk factors - the most frequent being cerebrovascular diseases, tumours and traumatic injuries. Several treatment options exist, including, for instance, pharmacotherapy, vagal nerve stimulation or epilepsy surgery. In spite of treatment, about 30% of patients with epilepsy still have seizures and become drug-refractory...
23, 2016: Annals of Agricultural and Environmental Medicine: AAEM
https://www.readbyqxmd.com/read/28025529/anticonvulsant-effects-of-fractions-isolated-from-dinoponera-quadriceps-kempt-ant-venom-formicidae-ponerinae
#18
Diana Aline Morais Ferreira Nôga, Luiz Eduardo Mateus Brandão, Fernanda Carvalho Cagni, Delano Silva, Dina Lilia Oliveira de Azevedo, Arrilton Araújo, Wagner Ferreira Dos Santos, Antonio Miranda, Regina Helena da Silva, Alessandra Mussi Ribeiro
Natural products, sources of new pharmacological substances, have large chemical diversity and architectural complexity. In this context, some toxins obtained from invertebrate venoms have anticonvulsant effects. Epilepsy is a neurological disorder that affects about 65 million people worldwide, and approximately 30% of cases are resistant to pharmacological treatment. Previous studies from our group show that the denatured venom of the ant Dinoponera quadriceps (Kempt) protects mice against bicuculline (BIC)-induced seizures and death...
December 23, 2016: Toxins
https://www.readbyqxmd.com/read/28024798/zonisamide-attenuates-lactacystin-induced-parkinsonism-in-mice-without-affecting-system-xc
#19
Eduard Bentea, Joeri Van Liefferinge, Lise Verbruggen, Katleen Martens, Sho Kobayashi, Lauren Deneyer, Thomas Demuyser, Giulia Albertini, Katrien Maes, Hideyo Sato, Ilse Smolders, Jan Lewerenz, Ann Massie
Zonisamide (ZNS), an anticonvulsant drug exhibiting symptomatic effects in Parkinson's disease (PD), was recently reported to exert neuroprotection in rodent models. One of the proposed neuroprotective mechanisms involves increased protein expression of xCT, the specific subunit of the cystine/glutamate antiporter system xc(-), inducing glutathione (GSH) synthesis. Here, we investigated the outcome of ZNS treatment in a mouse model of PD based on intranigral proteasome inhibition, and whether the observed effects would be mediated by system xc(-)...
December 24, 2016: Experimental Neurology
https://www.readbyqxmd.com/read/28018175/progressive-seizure-aggravation-in-the-repeated-6-hz-corneal-stimulation-model-is-accompanied-by-marked-increase-in-hippocampal-p-erk1-2-immunoreactivity-in-neurons
#20
Carmela Giordano, Anna M Costa, Chiara Lucchi, Giuseppina Leo, Luc Brunel, Jean-Alain Fehrentz, Jean Martinez, Antonio Torsello, Giuseppe Biagini
The 6-Hz corneal stimulation test is used to screen novel antiepileptic molecules to overcome the problem of drug refractoriness. Although recognized as a standard test, it has been evaluated only recently in the attempt to characterize the putative neuronal networks involved in seizures caused by corneal stimulation. In particular, by recording from the CA1 region we previously established that the hippocampus participates to propagation of seizure activity. However, these findings were not corroborated by using markers of neuronal activation such as FosB/ΔFosB antigens...
2016: Frontiers in Cellular Neuroscience
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