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https://www.readbyqxmd.com/read/29334622/pyridazinone-hybrids-design-synthesis-and-evaluation-as-potential-anticonvulsant-agents
#1
Sangh Partap, Md Jawaid Akhtar, Mohammed Shahar Yar, Mohd Zaheen Hassan, Anees Ahmad Siddiqui
A series of new hybrid benzothiazole containing pyridazinones derivatives were designed and synthesized fulfilling all the pharmacophoric requirements essential for the anticonvulsant activity. In-silico and in vitro studies revealed that some of these hybrid derivatives demonstrated admirable GABA AT inhibitory activity. An attempt has also been made to validate the results of in vitro GABA AT inhibition of the most potent compound SPS-5F (IC50 9.10 μM) through in vivo anticonvulsant screening. Compound SPS-5F administration significantly increases the whole brain GABA level, might be through the inhibition of GABA AT enzyme...
January 3, 2018: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29333826/vitamin-d-deficiency-in-pediatric-clinical-practice
#2
Gustavo Cediel, Johanna Pacheco-Acosta, Carlos CastiUo-Durdn
INTRODUCTION: Vitamin D research suggests it has a role in disorders other than bone metabolism. OBJECTIVE: To update the information on vitamin D deficiency (VDD) in pediatric clinical disorders. METHODS: Search in virtual libraries, giving priority to clinical and longitudinal studies and meta-analyses on VDD in the pediatric age group published in the past 20 years. The terms "vitamin D deficiency", "children and adolescents" (both in Spanish and English) were used as search descriptors...
February 1, 2018: Archivos Argentinos de Pediatría
https://www.readbyqxmd.com/read/29331845/effect-of-levetiracetam-on-extracellular-amino-acid-levels-in-the-dorsal-hippocampus-of-rats-with-temporal-lobe-epilepsy
#3
Pichardo Macías Luz Adriana, Ramírez Mendiola Blanca Alcira, Contreras García Itzel Jatziri, Zamudio Hernández Sergio Roberto, Chávez Pacheco Juan Luis, Sánchez Huerta Karla Berenice, Mendoza Torreblanca Julieta Griselda
Levetiracetam (LEV) is an anticonvulsant drug with a unique mechanism of action that is not completely understood. However, its activity profile may involve effects on excitatory and/or inhibitory neurotransmission since the primary target of LEV, synaptic vesicle protein 2A, is ubiquitously expressed in all types of synaptic vesicles. Therefore, the objective of the present study was to explore the effect of LEV (300 mg/kg/day for one week, administered via osmotic mini-pumps) on neurotransmitter release and its probable selective effect on extracellular gamma-amino butyric acid (GABA), glutamate (Glu), aspartate (Asp), glutamine (Gln), taurine (Tau) and glycine (Gly) concentrations (using in vivo microdialysis under basal and high-K+ conditions) in the dorsal hippocampus (DH), a region that undergoes major synaptic changes during epilepsy...
January 5, 2018: Epilepsy Research
https://www.readbyqxmd.com/read/29331789/anticonvulsant-activities-of-%C3%AE-asaronol-e-3-hydroxyasarone-an-active-constituent-derived-from-%C3%AE-asarone
#4
Xirui He, Yajun Bai, Min Zeng, Zefeng Zhao, Qiang Zhang, Ning Xu, Fanggang Qin, Xiaoyang Wei, Meimei Zhao, Ni Wu, Zehua Li, Yajun Zhang, Tai-Ping Fan, Xiaohui Zheng
BACKGROUND: Epilepsy is one of chronic neurological disorders that affects 0.5-1.0% of the world's population during their lifetime. There is a still significant need to develop novel anticonvulsant drugs that possess superior efficacy, broad spectrum of activities and good safety profile. METHODS: α-Asaronol and two current antiseizure drugs (α-asarone and carbamazepine (CBZ)) were assessed by in vivo anticonvulsant screening with the three most employed standard animal seizure models, including maximal electroshock seizure (MES), subcutaneous injection-pentylenetetrazole (PTZ)-induced seizures and 3-mercaptopropionic acid (3-MP)-induced seizures in mice...
August 31, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/29331765/5-6-dihydropyrimidine-1-2h-carbothioamides-synthesis-in-vitro-gaba-at-screening-anticonvulsant-activity-and-molecular-modelling-study
#5
Meeta Sahu, Nadeem Siddiqui, Vidushi Sharma, Sharad Wakode
Even after considerable advances in the field of epilepsy treatment, convulsions are inefficiently controlled by standard drug therapy. Herein, a series of pyrimidine-carbothioamide derivatives 4(a-t) was designed as anticonvulsant agents by doing some important structural modifications in well-known anticonvulsant drugs. Two classical animal models were used for the in vivo anticonvulsant screening, maximum electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ) models; followed by motor impairment study by rotarod method...
January 2, 2018: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29329017/amiodarone-a-multi-channel-blocker-enhances-anticonvulsive-effect-of-carbamazepine-in-the-mouse-maximal-electroshock-model
#6
Monika Banach, Monika Popławska, Kinga K Borowicz-Reutt
Cardiac arrhythmia may occur in the course of epilepsy. Simultaneous therapy of the two diseases might be complicated by drug interactions since antiarrhythmic and antiepileptic agents share some molecular targets. The aim of this study was to evaluate the influence of amiodarone, an antiarrhythmic drug working as a multi-channel blocker, on the protective activity of four classical antiepileptic drugs in the maximal electroshock test in mice. Amiodarone at doses up to 75 mg/kg did not affect the electroconvulsive threshold in mice...
January 5, 2018: Epilepsy Research
https://www.readbyqxmd.com/read/29325628/pharmacogenetics
#7
Jeffrey R Bishop
Pharmacogenetics is the study of how genetics influences drug treatment outcomes. Much research has been conducted to identify and characterize gene variants that impact the pharmacokinetic and pharmacodynamic aspects of medications used to treat neurologic and psychiatric disorders. This chapter reviews the current state of pharmacogenetic aspects of these treatments. Medications with supporting pharmacogenetic information in product labeling, clinical guidelines, or important mechanistic implications are discussed...
2018: Handbook of Clinical Neurology
https://www.readbyqxmd.com/read/29321995/anticonvulsant-effect-of-ethanolic-extract-of-cyperus-articulatus-l-leaves-on-pentylenetetrazol-induced-seizure-in-mice
#8
Oscar Herrera-Calderon, Rocio Santiváñez-Acosta, Bertha Pari-Olarte, Edwin Enciso-Roca, Vicente Martin Campos Montes, Jorge Luis Arroyo Acevedo
Cyperus articulatus (CA) rhizomes have demonstrated different properties on nervous system. However, the leaves still have not studied to treat epilepsy. The aim of this study was to determine the effect of CA ethanolic extract on pentylenetetrazol (PTZ) induced seizures in mice as well as measuring its antioxidant activity in vivo and in vitro. Mice were divided into five groups: (1) control (PTZ 80 mg/kg; i.p.), (2) PTZ-Diazepam (1 mg/kg; i.p.), (3-5) PTZ-CA 50, PTZ-CA 150 and PTZ-CA 300 (50, 150 and 300 mg/kg of CA extract, 30 min prior to each PTZ injection)...
January 2018: Journal of Traditional and Complementary Medicine
https://www.readbyqxmd.com/read/29320603/drug-management-for-acute-tonic-clonic-convulsions-including-convulsive-status-epilepticus-in-children
#9
REVIEW
Amy McTague, Timothy Martland, Richard Appleton
BACKGROUND: Tonic-clonic convulsions and convulsive status epilepticus (currently defined as a tonic-clonic convulsion lasting at least 30 minutes) are medical emergencies and require urgent and appropriate anticonvulsant treatment. International consensus is that an anticonvulsant drug should be administered for any tonic-clonic convulsion that has been continuing for at least five minutes. Benzodiazepines (diazepam, lorazepam, midazolam) are traditionally regarded as first-line drugs and phenobarbital, phenytoin and paraldehyde as second-line drugs...
January 10, 2018: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/29319453/evaluating-the-effectiveness-of-antidepressant-therapy-adjuvant-to-gabapentin-and-pregabalin-for-treatment-of-sci-related-neuropathic-pain
#10
Emily Carol McKinley, Elizabeth J Richardson, Gerald McGwin, Jie Zhang
OBJECTIVE: To investigate if a combination of anticonvulsant and antidepressant, two primary therapies for neuropathic pain, is associated with improved pain control compared to individual therapy. DESIGN: Prospective cohort study Setting: The University of Alabama at Birmingham Rehabilitation Center In-patient Program between 2012 and 2015. PARTICIPANTS: Incident SCI cases, 19-65 years of age. OUTCOMES: Bryce-Ragnarsson pain classification scheme and the Numerical Rating Scale Results: Twenty-nine eligible patients completed 6-month follow-up; their average age was 36...
January 10, 2018: Journal of Spinal Cord Medicine
https://www.readbyqxmd.com/read/29318288/green-one-pot-synthesis-of-novel-polysubstituted-pyrazole-derivatives-as-potential-antimicrobial-agents
#11
Hamid Beyzaei, Zahra Motraghi, Reza Aryan, Mohammad Mehdi Zahedi, Alireza Samzadeh-Kermani
Various biological properties of natural and synthetic pyrazole derivatives such as anti-inflammatory, antimicrobial, neuroprotective, anticonvulsant, antidepressant and anticancer activities encouraged us to propose a new, fast, green and eco-friendly procedure for the preparation of some novel 5-amino-3-(aryl substituted)-1-(2,4-dinitrophenyl)-1H-pyrazole-4-carbonitriles. They were efficiently synthesized via one-pot two-step process reaction of malononitrile, 2,4-dinitrophenylhydrazine and different benzaldehydes in deep eutectic solvent (DES) glycerol/potassium carbonate...
December 2017: Acta Chimica Slovenica
https://www.readbyqxmd.com/read/29303494/substituent-position-effect-on-the-crystal-structures-of-n-phenyl-2-phthalimidoethanesulfonamide-derivatives
#12
Resul Sevinçek, Duygu Barut Celepci, Serap Köktaş Koca, Özlem Akgül, Muittin Aygün
In order to determine the impact of different substituents and their positions on intermolecular interactions and ultimately on the crystal packing, unsubstituted N-phenyl-2-phthalimidoethanesulfonamide, C16H14N2O4S, (I), and the N-(4-nitrophenyl)-, C16H13N3O6S, (II), N-(4-methoxyphenyl)-, C16H16N3O6S, (III), and N-(2-ethylphenyl)-, as the monohydrate, C18H18N2O4S·H2O, (IV), derivatives have been characterized by single-crystal X-ray crystallography. Sulfonamides (I) and (II) have triclinic crystal systems, while (III) and (IV) are monoclinic...
January 1, 2018: Acta Crystallographica. Section C, Structural Chemistry
https://www.readbyqxmd.com/read/29302750/decreased-plasma-agmatine-levels-in-autistic-subjects
#13
Erman Esnafoglu, İlhan İrende
Agmatine is a polyamine endogenously synthesized from arginine and is considered to be a new neurotransmitter. Agmatine has been implicated in the pathophysiology of several diseases such as anxiety disorder, depression, and schizophrenia. Agmatine also possesses anticonvulsant, neuroprotective, antiapoptotic, antioxidant, anxiolytic, and antidepressant effects. Furthermore, agmatine inhibits the nitric oxide synthase enzyme and exerts antagonist effects on NMDA, alpha-2, and imidazoline receptors. Considering these characteristics, the present study investigated whether agmatine plays a role in the pathogenesis of autistic spectrum disorders (ASDs)...
January 4, 2018: Journal of Neural Transmission
https://www.readbyqxmd.com/read/29301160/-pharmacotherapy-of-vestibular-disorders-nystagmus-and-cerebellar-disorders
#14
K Feil, N Böttcher, O Kremmyda, C Muth, J Teufel, A Zwergal, T Brandt, M Strupp
There are currently different groups of drugs for the pharmacotherapy of vertigo, nystagmus and cerebellar disorders: antiemetics; anti-inflammatories, antimenieres, and antimigraineous medications and antidepressants, anticonvulsants, aminopyridines as well as acetyl-DL-leucine. In acute unilateral vestibulopathy, corticosteroids improve the recovery of peripheral vestibular function, but currently there is not sufficient evidence for a general recommendation. There is insufficient evidence to support the view that 16 mg t...
January 2018: Laryngo- Rhino- Otologie
https://www.readbyqxmd.com/read/29298039/isatin-detection-using-a-boron-doped-diamond-3-in-1-sensing-platform
#15
Mary Ensch, Vanessa Y Maldonado, Greg M Swain, Robert Rechenberg, Michael F Becker, Thomas Schuelke, Cory A Rusinek
Boron-doped diamond (BDD) is a promising electrochemical tool that exhibits excellent chemical sensitivity and stability. These intrinsic advantages coupled with the material's vast microfabrication flexibility make BDD an attractive sensing device. In this study, two different 3-in-1 BDD electrode sensors were fabricated, characterized, and investigated for their capability to detect isatin, an anxiogenic indole that possesses anticonvulsant activity. Each device is comprised of a working, reference, and auxiliary electrode, all made of BDD...
January 3, 2018: Analytical Chemistry
https://www.readbyqxmd.com/read/29297810/sarcocystis-neurona-associated-meningoencephalitis-in-a-pacific-walrus-odobendus-rosmarus-divergens
#16
Lana Krol, Vanessa Fravel, Diana G Procter, Kathleen M Colegrove
A 21-yr-old intact male walrus ( Odobendus rosmarus divergens) presented with acute onset of shifting lameness, initially associated with breeding behaviors. Further clinical signs manifested, including muscle tremors, anorexia, hematuria, and coughing. Diagnostics were limited, as the animal would not offer behaviors for voluntary sample collection. Signs were addressed with anti-inflammatories, anticonvulsants, and antibiotics. The walrus developed cluster seizures and ultimately, respiratory and cardiac arrest...
December 2017: Journal of Zoo and Wildlife Medicine: Official Publication of the American Association of Zoo Veterinarians
https://www.readbyqxmd.com/read/29289486/posterior-reversible-encephalopathy-syndrome-following-blood-transfusion-in-a-patient-with-factor-x-deficiency-is-it-an-unusual-systemic-manifestation-of-an-adverse-transfusion-reaction
#17
Anupam Verma, Hemlata, Priti Elhence, Shubha R Phadke, Zafar Neyaz
Adverse neurological transfusion reactions including posterior reversible encephalopathy syndrome (PRES) following blood transfusion are rare. Our case an 18-year-female with known Factor X deficiency with menorrhagia developed severe hypertension, followed by generalised tonic clonic convulsions apparently after blood component transfusion. She had earlier received 4 units of red blood cells (RBC) for anaemia and 10 units of fresh frozen plasma (FFP) for menorrhagia (with prolonged PT and APTT) within short span of time at another hospital...
December 6, 2017: Transfusion and Apheresis Science
https://www.readbyqxmd.com/read/29286538/effect-of-gabapentin-on-sleep-and-event-related-oscillations-eros-in-rats-exposed-to-chronic-intermittent-ethanol-vapor-and-protracted-withdrawal
#18
Manuel Sanchez-Alavez, Derek N Wills, Leslie Amodeo, Cindy L Ehlers
Disturbances in sleep architecture, especially reductions in slow wave sleep (SWS), are symptoms commonly observed in individuals with alcohol use disorders (AUDs). Recent clinical trials have demonstrated that the anticonvulsant and analgesic drug Gabapentin may have therapeutic value in normalizing sleep quality in recovering alcoholics. However, the brain mechanisms underlying this improvement in sleep following Gabapentin treatment remain unknown METHODS: In the present study, adult Wistar rats were exposed to 8 weeks of chronic intermittent ethanol vapor (CIE) (blood ethanol concentrations averaged 128...
December 29, 2017: Alcoholism, Clinical and Experimental Research
https://www.readbyqxmd.com/read/29286347/anticonvulsant-activity-of-halogen-substituted-cinnamic-acid-derivatives-and-their-effects-on-glycosylation-of-ptz-induced-chronic-epilepsy-in-mice
#19
Ye Cuan, Xirui He, Yuhui Zhao, Jiajun Yang, Yajun Bai, Yin Sun, Qiang Zhang, Zefeng Zhao, Xiaoyang Wei, Xiaohui Zheng
Epilepsy is a common chronic neurological disorder disease, and there is an urgent need for the development of novel anticonvulsant drugs. In this study, the anticonvulsant activities and neurotoxicity of 12 cinnamic acid derivatives substituted by fluorine, chlorine, bromine, and trifluoromethyl groups were screened by the maximal electroshock seizure (MES) and rotarod tests (Tox). Three of the tested compounds (compounds 3, 6 and 12) showed better anticonvulsant effects and lower neurotoxicity. They showed respective median effective dose (ED50) of 47...
December 29, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29285684/socioeconomic-disparities-and-metabolic-risk-in-veterans-with-serious-mental-illness
#20
Stanley N Caroff, Shirley H Leong, Daisy Ng-Mak, E Cabrina Campbell, Rosalind M Berkowitz, Krithika Rajagopalan, Chien-Chia Chuang, Antony Loebel
Socioeconomic disparities were assessed in predicting metabolic risk among veterans with serious mental illness. Veterans with schizophrenia, schizoaffective, or bipolar disorders were identified in VISN 4 facilities from 10/1/2010 to 9/30/2012. Differences between patients with and without metabolic syndrome were compared using t-tests, Chi square tests and multivariate logistic regressions. Among 10,132 veterans with mental illness, 48.8% had metabolic syndrome. Multivariate logistic regression analysis confirmed that patients with metabolic syndrome were significantly more likely to be older, male, African-American, married, and receiving disability pensions but less likely to be homeless...
December 28, 2017: Community Mental Health Journal
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