Search results for " Valproic acid"

showing 5 items of 5 documents

Valproate and Short-Chain Fatty Acids Activate Transcription of the Human Vitamin D Receptor Gene through a Proximal GC-Rich DNA Region Containing Tw…

2022

The vitamin D receptor (VDR) mediates 1,25-dihydroxyvitamin D3 pleiotropic biological actions through transcription regulation of target genes. The expression levels of this ligand-activated nuclear receptor are regulated by multiple mechanisms both at transcriptional and post-transcriptional levels. Vitamin D3 is the natural VDR activator, but other molecules and signaling pathways have also been reported to regulate VDR expression and activity. In this study, we identify valproic acid (VPA) and natural short-chain fatty acids (SCFAs) as novel transcriptional activators of the human VDR (hVDR) gene. We further report a comprehensive characterization of VPA/SCFA-responsive elements in the 5…

BioquímicaBiologiaVDR induction; human VDR promoter; valproic acid; SCFA; Sp1.Binding SitesNutrition and DieteticsSp1 Transcription FactorValproic AcidDNAHumansReceptors Calcitriollipids (amino acids peptides and proteins)ChildPromoter Regions GeneticFood Science
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N-valproyl-L-tryptophan for CNS-targeting: synthesis, characterization and efficacy in vitro studies of a new potential antiepileptic drug.

2010

A new aminoacidic derivative of valproic acid (VPA) has been synthesized and characterized by analytical and spectral data. The rationale for the preparation of such potential antiepileptic agent is based on the observation that chemical combination of the anticonvulsant pharmacophore, VPA with essential aminoacids could afford more effective and less toxic actives. The synthesis, characterization, physico-chemical parameters functional for crossing Blood Brain Barrier of N-valproyl-L-tryptophan (4) are reported. The Log D pH7.4 (0.3) indicates that (4) is adequate to cross biological membranes. Its chemical and enzymatic stability were assessed. The experiments indicate high stability of c…

Malemedicine.medical_treatmentHippocampal formationPharmacologyIn Vitro TechniquesBlood–brain barrierSettore BIO/09 - FisiologiaHippocampuschemistry.chemical_compoundDrug StabilityIn vivoDrug DiscoverymedicineAnimalsRats WistarValproic AcidEpilepsyDipeptidesAminoacidic derivative Antiepileptic Drug CNS-Targeting Enzymatic Stability Seizure Like Events Model Valproic acidIn vitroElectrophysiological PhenomenaRatsmedicine.anatomical_structureAnticonvulsantchemistrySettore CHIM/09 - Farmaceutico Tecnologico ApplicativoAnticonvulsantsPharmacophoreDerivative (chemistry)medicine.drugMedicinal chemistry (Shariqah (United Arab Emirates))
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Rufinamide in children and adults with Lennox-Gastaut syndrome: first Italian multicenter experience

2010

This is the first multicenter Italian experience with rufinamide as an adjunctive drug in children, adolescents and adults with Lennox-Gastaut syndrome. The patients were enrolled in a prospective, add-on, open-label treatment study from 11 Italian centers for children and adolescent epilepsy care. Forty-three patients (26 males, 17 females), aged between 4 and 34 years (mean 15.9 ± 7.3, median 15.0), were treated with rufinamide for a mean period of 12.3 months (range 3-21 months). Twenty patients were diagnosed as cryptogenic and 23 as symptomatic. Rufinamide was added to the baseline therapy at the starting dose of 10mg/kg body weight, evenly divided in two daily doses and then increased…

MalePediatricsLennox-Gastaut syndromeAtypical absence seizuresRufinamideLennox–Gastaut syndrome; Rufinamide; Orphan drug; Pediatrics; Epilepsy; Drop attacksInfantilePediatricsSpasmsEpilepsyRufinamideDrop attacks; Epilepsy; Lennox-Gastaut syndrome; Orphan drug; Pediatrics; Rufinamide; Adolescent; Adult; Anticonvulsants; Child; Child Preschool; Drug Therapy Combination; Female; Humans; Intellectual Disability; Italy; Lennox Gastaut Syndrome; Male; Spasms Infantile; Treatment Outcome; Triazoles; Valproic Acid; Young Adult; Neurology (clinical); NeurologyChildPediatricValproic AcidDrop attacksGeneral MedicineSettore MED/39 - Neuropsichiatria InfantileTreatment OutcomeItalyNeurologyAnesthesiaChild PreschoolCombinationVomitingAnticonvulsantsDrug Therapy CombinationFemalemedicine.symptomSpasms Infantilemedicine.drugAdultmedicine.medical_specialtyAdolescentClinical NeurologyIrritabilityYoung AdultDrug TherapyIntellectual DisabilitymedicineHumanspediatrics epilepsyPreschoolAdverse effectLennox–Gastaut syndrome; rufinamide; orphan drug; pediatrics epilepsy; drop attacks; refractory epilepsy.EpilepsyOrphan drugbusiness.industryLennox Gastaut SyndromeValproic Acidrefractory epilepsyTriazolesmedicine.diseaseNeurology (clinical)businessLennox–Gastaut syndromeLennox–Gastaut syndrome
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N-Valproyl-L-Phenylalanine as new potential antiepileptic drug: Synthesis, characterization and in vitro studies on stability, toxicity and anticonvu…

2013

Valproic acid (VPA) is considered first-line drug in treatment of generalized idiopathic seizures such as absence, generalized tonic-clonic and myoclonic seizures. Among major antiepileptic drugs, VPA is also considered effective in childhood epilepsies and infantile spasms. Due to its broad activity, VPA acts as a mood stabilizer in bipolar disorder and it is useful in migraine prophylaxis. Despite its long-standing usage, severe reactions to VPA, such as liver toxicity and teratogenicity, are reported. To circumvent side effects due to structural characteristics of VPA, we synthesized in good yield a new VPA-aminoacid conjugate, the N-valproyl-L-Phenylalanine, and characterized by FT-IR, …

MaleDrugCell Membrane PermeabilityAminoacidic derivative Astrocytes toxicity CNS-Targeting Enzymatic Stability Hippocampal epilepsy Valproic acid.Cell Survivalmedicine.drug_classPhenylalaninemedicine.medical_treatmentmedia_common.quotation_subjectPrimary Cell CulturePhenylalaninePharmacologySettore BIO/09 - FisiologiaHippocampusTissue Culture TechniquesDrug StabilityDrug DiscoverymedicineAnimalsRats WistarEvoked Potentialsmedia_commonValproic AcidChemistryHydrolysisValproic AcidBiological TransportMood stabilizerMicrotomyHydrogen-Ion ConcentrationIn vitroRatsAnticonvulsantSettore CHIM/09 - Farmaceutico Tecnologico ApplicativoAstrocytesToxicityAnticonvulsantslipids (amino acids peptides and proteins)Conjugatemedicine.drug
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Inhibitory effects of N-valproyl-L-tryptophan on high potassium, low calcium and low magnesium-induced CA1 hippocampal epileptiform bursting activity…

2012

N-valproyl-l-tryptophan (VPA-Tryp), new antiepileptic drug, was tested on CA1 hippocampal epileptiform bursting activity obtained by increasing potassium and lowering calcium and magnesium concentrations in the fluid perfusing rat brain slices. Each slice was treated with a single concentration (0.2, 0.5, 1 or 2 mM) of Valproate (VPA) or VPA-Tryp. Both burst duration and interburst frequency during and after treatment were off-line compared with baseline values. For both parameters, the latency and the length of statistically significant response periods as well as the magnitude of drug-induced responses were calculated. VPA-Tryp evoked fewer and weaker early excitatory effects than VPA on …

Maleantiepileptic drug valproic acidPotassiumchemistry.chemical_elementAction PotentialsCalciumHippocampal formationPharmacologyIn Vitro TechniquesInhibitory postsynaptic potentialSettore BIO/09 - Fisiologiaamino-acidic derivativeBurstingmedicineReaction Timehippocampal epilepsyAnimalsDrug InteractionsMagnesiumRats WistarCA1 Region HippocampalBiological PsychiatryValproic AcidAnalysis of VarianceDose-Response Relationship DrugMagnesiumDipeptidesElectric StimulationRatsPsychiatry and Mental healthNeurologychemistrySettore CHIM/09 - Farmaceutico Tecnologico ApplicativoExcitatory postsynaptic potentialPotassiuminterictal burstslipids (amino acids peptides and proteins)AnticonvulsantsNeurology (clinical)medicine.drugJournal of neural transmission (Vienna, Austria : 1996)
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