Search results for "Glutamate receptor antagonist"

showing 4 items of 4 documents

Dose escalating safety study of CNS 5161 HCl, a new neuronal glutamate receptor antagonist (NMDA) for the treatment of neuropathic pain

2007

What is already known about this subject • Despite encouraging effects of N-methyl-D-aspartate (NMDA) receptor antagonists in reducing neuropathic pain of different aetiologies, the clinical use of these agents has been limited by their mainly psychotropic side-effects. • In a recent study in healthy volunteers, CNS 5161, a novel noncompetetive NMDA receptor antagonist, was well tolerated up to a dosage of 2000 µg without psychotropic side-effects. • This is the first study to evaluate the maximal tolerated dosage of CNS 5161 and to gain experience about the analgesic effect of CNS 5161 in patients with different pain syndromes. What this study adds • In patients with neuropathic pain CNS 5…

AdultMaleVisual analogue scaleAnalgesicPlaceboGuanidinesReceptors N-Methyl-D-Aspartatechemistry.chemical_compoundDrug SafetyDouble-Blind MethodMedicineHumansPharmacology (medical)Glutamate receptor antagonistSulfhydryl CompoundsAdverse effectAgedPain MeasurementPharmacologyCross-Over StudiesDose-Response Relationship Drugbusiness.industryTherapeutic effectMiddle AgedBlood pressurechemistryAnesthesiaNeuropathic painNeuralgiaFemalebusiness
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Effect of memantine and CNQX in the acquisition, expression and reinstatement of cocaine-induced conditioned place preference

2006

The present study evaluates the effect of memantine, a non-competitive N-methyl-d-aspartate (NMDA) glutamate receptor antagonist and CNQX, an alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA)/kainate receptor antagonist on the rewarding effects of cocaine in mice, using the conditioned place preference (CPP) paradigm. Cocaine-induced CPP was studied pairing this drug with different memantine or CNQX doses during either the acquisition or the expression phase of the procedure. Once CPP was established, and the preference extinguished, reinstatement was induced by a priming dose of cocaine. Both antagonists, which in themselves do not present motivational actions on the preferen…

MaleKainate receptorAMPA receptorPharmacologyExtinction PsychologicalMicechemistry.chemical_compoundCocaineDopamine Uptake InhibitorsMemantineAnimalsMedicineDrug InteractionsGlutamate receptor antagonistBiological Psychiatry6-Cyano-7-nitroquinoxaline-23-dionePharmacologyBehavior AnimalDose-Response Relationship Drugbusiness.industryGlutamate receptorMemantineConditioned place preferencenervous systemchemistryCNQXConditioning OperantNMDA receptorbusinessExcitatory Amino Acid AntagonistsReinforcement Psychologypsychological phenomena and processesmedicine.drugProgress in Neuro-Psychopharmacology and Biological Psychiatry
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Optimization of a LC method for the enantioseparation of a non-competitive glutamate receptor antagonist, by experimental design methodology

2006

Abstract The aim of this work was to obtain the direct optical resolution of a new glutamate receptor antagonist (( p -chloro)1-aryl-6,7,-dimethoxy-1,2,3,4-tetrahydroisoquinoline, PS3), by liquid chromatography on Chiralcel ® OD column. A response surface methodology (RSM) was employed to optimize the enantiomeric separation of the racemate with the lowest number of experiments; in particular, a face-centred design (FCD) was applied to evaluate the influence of critical parameters on the experimental response. Furthermore, in order to find the best compromise between several responses, a multicriteria decision-making approach, the Derringer's desirability function, was successful to simulta…

Resolution (mass spectrometry)Clinical BiochemistryAnalytical chemistryPharmaceutical ScienceChiral liquid chromatography Enantioresolution Chiralcel® OD Tetrahydroisoquinoline derivative Face-centred design Desirability functionHigh-performance liquid chromatographyAnalytical Chemistrychemistry.chemical_compoundTetrahydroisoquinolinesDrug DiscoveryGlutamate receptor antagonistResponse surface methodologySpectroscopyChiral liquid chromatographyChromatographyMolecular StructureAntagonistChiralcel® ODStereoisomerismTetrahydroisoquinoline derivativeDesirability functionFace-centred designHexanechemistryModels ChemicalDesirability functionEnantiomerEnantioresolutionExcitatory Amino Acid AntagonistsChromatography Liquid
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Perampanel and Visuospatial Skills in Children With Epilepsy

2021

Introduction: Perampanel (PER) is a non-competitive AMPA glutamate receptor antagonist approved for focal and generalized seizures as add-on therapy. PER does not seem to negatively affect the cognitive profile in children and adolescents, but its influence on visuospatial abilities is still to be assessed. The aim of our study was to assess visuospatial skills through a standardized neuropsychological evaluation in adolescents taking PER for 12 months.Methods: Our sample included 46 adolescents aged 12–18 years with focal and generalized drug-resistant epilepsy already in therapy with one or two antiseizure medications. Changes in visuospatial perception and memory were assessed by the Rey…

medicine.medical_specialtygenetic structuresAudiologybehavioral disciplines and activitiesSpatial memory050105 experimental psychology03 medical and health sciencesPerampanelchemistry.chemical_compound0302 clinical medicineperampanelchildrenmedicineadverse effects children perampanel tolerability visuospatial memory0501 psychology and cognitive sciencesGlutamate receptor antagonisttolerabilityRC346-429Original Researchbusiness.industry05 social sciencesNeuropsychologyCognitionExecutive functionsNeurologychemistryVisuospatial perceptionAdjunctive treatmentadverse effectsvisuospatial memoryNeurology. Diseases of the nervous systemNeurology (clinical)business030217 neurology & neurosurgery
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