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Selwyn S Jayakar et al.
Molecular pharmacology, 95(6), 615-628 (2019-04-07)
GABAA receptors (GABAARs) are targets for important classes of clinical agents (e.g., anxiolytics, anticonvulsants, and general anesthetics) that act as positive allosteric modulators (PAMs). Previously, using photoreactive analogs of etomidate ([3H]azietomidate) and mephobarbital [[3H]1-methyl-5-allyl-5-(m-trifluoromethyl-diazirynylphenyl)barbituric acid ([3H]R-mTFD-MPAB)], we identified two homologous
Behrouz Kassaï et al.
Epilepsia, 49(2), 343-348 (2007-11-22)
Severe myoclonic epilepsy in infancy (SMEI) is a rare, but severe disorder with seizures typically resistant to conventional antiepileptic drugs. The objective of the present study was to systematically review the literature on the available treatments for SMEI. Databases searched
Jarogniew J Luszczki et al.
Epilepsy research, 90(3), 188-198 (2010-05-25)
The aim of this study was to characterize the anticonvulsant effects of stiripentol (STP) in combination with clobazam [CLB], and valproate [VPA]) in the mouse maximal electroshock (MES)-induced seizure model using the type I isobolographic analysis for parallel and non-parallel
Milena Djuric et al.
Epileptic disorders : international epilepsy journal with videotape, 13(1), 22-26 (2011-03-12)
The syndrome of malignant migrating partial seizures in infancy is a devastating, age-specific, epileptic encephalopathy, which still presents an aetiological, pathophysiological and therapeutic problem. In this study, we present two patients who were diagnosed with the disease, based on electroclinical
Screening of conventional anticonvulsants in a genetic mouse model of epilepsy.
Hawkins NA, et al.
Annals of Clinical and Translational Neurology, 4(5), 326-339 (2017)
Marie-Clémence Verdier et al.
Therapie, 67(2), 157-160 (2012-08-02)
Stiripentol is a third generation antiepileptic, marketed since 2007 under the name of Diacomit(®). It is indicated, always in combination, in the treatment of severe myoclonic epilepsy in infancy or Dravet syndrome. Its pharmacokinetics is not linear. It is a
Catherine Chiron
Expert opinion on investigational drugs, 14(7), 905-911 (2005-07-19)
Stiripentol (STP) is a new antiepileptic compound produced by Biocodex. It is not structurally related to any of the other currently marketed antiepileptic products as it belongs to the group of aromatic allylic alcohols. It has recently been proved to
Jarogniew J Luszczki et al.
Epilepsia, 47(11), 1841-1854 (2006-11-23)
Isobolographic analysis was used to characterize the interactions between stiripentol (STP) and clonazepam (CZP), ethosuximide (ETS), phenobarbital (PB), and valproate (VPA) in suppressing pentylenetetrazole (PTZ)-induced clonic seizures in mice. The anticonvulsant and acute adverse (neurotoxic) effects of STP in combination
M Bebin et al.
Drugs, 48(2), 153-171 (1994-08-01)
In the past decade, several new antiepileptic drugs have been tested. Most recently, 5 new antiepileptic drugs have been launched onto European and US markets. These include vigabatrin, oxcarbazepine and lamotrigine in Europe, and felbamate and gabapentin in the US.
Carole Giraud et al.
Drug metabolism and disposition: the biological fate of chemicals, 34(4), 608-611 (2006-01-18)
A metabolic interaction between stiripentol (STP), an anticonvulsant agent that inhibits the activity of several cytochromes P450 (P450s), and clobazam (CLB), a 1,5-benzodiazepine, used in association with STP in severe myoclonic epilepsy in infancy was observed in vivo. This interaction
C Chiron et al.
Lancet (London, England), 356(9242), 1638-1642 (2000-11-23)
Stiripentol is an inhibitor of cytochrome P450 that showed antiepileptic efficacy in severe myoclonic epilepsy in infancy (SMEI) in association with clobazam and valproate in an open study. To confirm these results, 41 children with SMEI were included in a
Catherine Chiron
Neurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics, 4(1), 123-125 (2007-01-03)
Stiripentol (STP) is a new antiepileptic compound made by Biocodex. It recently proved to increase the GABAergic transmission in vitro in an experimental model of immature rat. Clinical studies were based on the fact that STP also acts as an
Greg L Plosker
CNS drugs, 26(11), 993-1001 (2012-09-29)
Stiripentol is an anticonvulsant used as adjunctive therapy with valproate and clobazam in the management of patients with severe myoclonic epilepsy of infancy (SMEI; Dravet syndrome), a rare form of epilepsy that develops in the first year of life and
Mohamed N Aboul-Enein et al.
European journal of medicinal chemistry, 47(1), 360-369 (2011-11-29)
A series of stiripentol (STP) analogues namely, 2-[(1E)-1-(1,3-benzodioxol-5-yl)-4,4-dimethylpent-1-en-3-ylidene]-N-(aryl/H)hydrazinecarboxamides 7a-h, (±)-(5RS)-N-(aryl/H)-(1,3-benzodioxol-5-yl)-3-tert-butyl-4,5-dihydro-1H-pyrazole-1-carboxamides (±)-8a-h, and (±)-[(5RS)-(1,3-benzodioxol-5-yl)-3-tert-butyl-4,5-dihydro-1H-pyrazol-1-yl](aryl)methanones (±)-13a-f was synthesized by adopting appropriate synthetic routes and was pharmacologically evaluated in the preliminary anticonvulsant screens. The selected bioactive new chemical entities were subjected to ED(50)
HIGHLY SENSITIVE SYNCHRONOUS SPECTROFLUORIMETRIC METHOD FOR DETERMINATION OF STIRIPENTOL IN CAPSULES AND HUMAN URINE: APPLICATION TO IN-VITRO DRUG RELEASE AND WEIGHT VARIATION TEST.
Darwish HW, et al.
Digest Journal of Nanomaterials and Biostructures, 9(2), 819-829 (2014)
Zsuzsa Siegler et al.
Ideggyogyaszati szemle, 61(11-12), 402-408 (2008-12-17)
Severe myoclonic epilepsy in infancy (SMEI; Dravet's syndrome) is a malignant epilepsy syndrome characterized by prolonged febrile hemiconvulsions or generalized seizures starting in the first year of life. Later on myoclonic, atypical absence, and complex partial seizures appear. When one
Jarogniew J Luszczki et al.
Naunyn-Schmiedeberg's archives of pharmacology, 374(1), 51-64 (2006-09-15)
The anticonvulsant effects produced by stiripentol (STP), carbamazepine (CBZ), and their combination in the maximal electroshock (MES)-induced seizures in mice were investigated using three-dimensional (3D) isobolographic analysis. With 3D isobolography, the combinations of both drugs at the fixed-ratios of 1:3
Elaine C Wirrell et al.
Epilepsia, 54(9), 1595-1604 (2013-07-16)
To review the efficacy and tolerability of stiripentol in the treatment of U.S. children with Dravet syndrome. U.S. clinicians who had prescribed stiripentol for two or more children with Dravet syndrome between March 2005 and 2012 were contacted to request
The new antiepileptic drugs.
S Macleod et al.
Archives of disease in childhood. Education and practice edition, 92(6), 182-188 (2007-11-23)
Theodor W May et al.
Therapeutic drug monitoring, 34(4), 390-397 (2012-06-30)
Stiripentol (STP) was approved as an orphan drug in 2007 in Europe as adjunctive therapy with valproic acid (VPA) and clobazam (CLB) for Dravet syndrome. Dravet syndrome is a highly pharmacoresistant form of epilepsy, which starts in early childhood. Data
Pascale P Quilichini et al.
Epilepsia, 47(4), 704-716 (2006-05-03)
Stiripentol (STP) is currently an efficient drug for add-on therapy in infantile epilepsies because it improves the efficacy of antiepileptic drugs (AEDs) through its potent inhibition of liver cytochromes P450. In addition, STP directly reduces seizures in several animal models
Acute hepatic injury in a child with Dravet syndrome: no protective effect of stiripentol.
Joanne F Goorhuis et al.
Seizure, 17(5), 477-478 (2008-04-11)
Rima Nabbout et al.
European journal of paediatric neurology : EJPN : official journal of the European Paediatric Neurology Society, 16 Suppl 1, S13-S17 (2012-06-15)
The efficacy of stiripentol (STP) in Dravet Syndrome (DS) was discovered first in an exploratory study in pediatric pharmacoresistant epilepsies. This efficacy signal, used as a proof of concept, led to - two independent multicenter randomized, double-blind, placebo-controlled trials in
Janet L Fisher
Epilepsia, 52 Suppl 2, 76-78 (2011-04-08)
The anticonvulsant stiripentol (Diacomittm) has been shown to have a positive impact on control of seizures for many patients with Dravet syndrome. As with most antiepileptic drugs, stiripentol has multiple mechanisms of action. Its direct anticonvulsant activity is likely due
Janet L Fisher
European journal of pharmacology, 654(2), 160-165 (2011-01-18)
Many patients with refractory epilepsy are treated with polytherapy, and nearly 15% of epilepsy patients receive two or more anti-convulsant agents. The anti-convulsant stiripentol is used as an add-on treatment for the childhood epilepsy syndrome known as severe myoclonic epilepsy
Stéphane Auvin et al.
Epilepsia, 54(12), 2082-2090 (2013-10-15)
After the first positive experimental data in rodents in the early 1970s demonstrating the anticonvulsant effect of stiripentol (STP), in vitro studies showed that STP acts directly on γ-aminobutyric acid A (GABAA ) receptors. Chloride influx is higher when these
Stiripentol.
J C Vincent
Epilepsy research. Supplement, 3, 153-156 (1991-01-01)
Catherine Chiron et al.
Journal of child neurology, 21(6), 496-502 (2006-09-05)
Stiripentol, a new antiepileptic drug inhibiting cytochrome P450-enzymes, suggested some efficacy when combined with carbamazepine in an open trial in refractory partial epilepsy of childhood. Our objective was to test these results in a placebo-controlled trial. To limit the number
Ernestina Marianna De Francesco et al.
Oncotarget, 8(40), 67269-67286 (2017-10-06)
Here, we developed a new synthetic lethal strategy for further optimizing the eradication of cancer stem cells (CSCs). Briefly, we show that chronic treatment with the FDA-approved antibiotic Doxycycline effectively reduces cellular respiration, by targeting mitochondrial protein translation. The expression
Michał K Trojnar et al.
Pharmacological reports : PR, 57(2), 154-160 (2005-05-12)
Epilepsy is one of the most widespread pathologies of human brain, affecting approximately 1% of world population. Despite the development of new methods of seizure control, chronic administration of antiepileptic drugs (AEDs) remains the treatment of choice. Nevertheless, pharmacotherapy is
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