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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
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
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
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
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
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
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
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)
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
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)
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
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.
Rima Nabbout et al.
Epilepsia, 52(7), e54-e57 (2011-05-17)
We aimed to test the efficacy of ketogenic diet (KD) in patients with Dravet syndrome (DS) not satisfactorily controlled by antiepileptic drugs (AEDs). We included prospectively 15 DS patients aged >3 years with partial response to AEDs including stiripentol. All
Xingwang Zhang et al.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, 62, 301-308 (2014-06-24)
Oral delivery of many drugs is plagued with limited solubility and/or poor stability. This paper aimed to explore the performance of polymeric mixed micelles on solubilization, stabilization and bioavailability enhancement with stiripentol as model drug. Stiripentol-loaded mixed micelles were prepared
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
Paolo Prunetti et al.
Current opinion in neurology, 24(2), 159-164 (2011-02-09)
There is a need for newer anti-epileptic drugs (AEDs) with improved efficacy and tolerability. This article reviews AEDs introduced since 2007 and investigational compounds in clinical development. Two recently introduced AEDs, stiripentol and rufinamide, have been licensed exclusively for orphan
J Kröll-Seger et al.
Neuropediatrics, 37(6), 325-329 (2007-03-16)
The purpose of this study was to assess the effectiveness and tolerability of topiramate (TPM) as add-on therapy in children with Dravet syndrome and considered unsatisfactorily controlled using stiripentol. All the 36 patients having been treated with TPM in our
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
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
Stiripentol.
J C Vincent
Epilepsy research. Supplement, 3, 153-156 (1991-01-01)
Dezhi Cao et al.
Epilepsia, 53(7), 1140-1145 (2012-05-15)
We previously reported a mutant mouse carrying a severe myoclonic epilepsy in infancy (SMEI) mutation in Scn1a. In this study, we examined the susceptibility to hyperthermia-induced seizures of heterozygous Scn1a mutant mice (Scn1a(RX/+)) and wild-type (Scn1a(+/+) ) mice. Then we
Dana Merdariu et al.
Brain & development, 35(2), 177-180 (2012-04-24)
The syndrome of malignant migrating partial seizures of infancy (MMPSI) is characterized by early onset of multiple seizure types and overall poor prognosis. Seizures are markedly drug resistant and few reports have suggested the efficacy of some antiepileptic drugs. We
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
Yushi Inoue et al.
Epilepsia, 50(11), 2362-2368 (2009-06-26)
To survey the treatment situation of Dravet syndrome in Japan and to compare this result with effectiveness of stiripentol (STP) add-on therapy in an open-label multicenter study. Medical records of patients with Dravet syndrome who visited the study institutions during
Catherine Chiron
Developmental medicine and child neurology, 53 Suppl 2, 16-18 (2011-04-29)
Dravet syndrome is a highly pharmaco-resistant form of epilepsy. Valproate and benzodiazepines are the first-line treatment but are usually insufficient therapeutic options. Lamotrigine, carbamazepine and high doses of intravenous phenobarbital can aggravate seizures and should be avoided. Topiramate, levetiracetam, bromide
Atsushi Fujiwara et al.
Journal of anesthesia, 34(3), 373-381 (2020-03-20)
Antiepileptic drugs are used not only for the treatment of epilepsy but also for that of neuropathic pain. However, their action mechanisms have not always been well explained. Stiripentol, an effective antiepileptic drug indicated as a therapeutic for Dravet syndrome
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