Search results for "Nitrazepam"

showing 10 items of 18 documents

The Effect of Nitrazepam on Manual Skill, Grip Strength, and Reaction Time with Special Reference to Subjective Evaluation of Effects on Sleep

1978

The effects of 5 and 10 mg oral nitrazepam doses on manual skills, grip strength, and reaction time 8 hours after ingestion of the drugs were studied in 34 healthy female volunteers aged 19-22 years. 5 mg nitrazepam caused a slight but insignificant decrease in psychomotor skills. With 10 mg psychomotor skills were influenced significantly. Grip strength and reaction time were not influenced either by the 5 or 10 mg doses. The investigators corroborate the value of the established effects of nitrazepam as a hypnotic, but recommend that caution should be excercised in prescribing the drug as a hypnotic (especially in doses exceeding 5 mg) to work-aged subjects as there is a risk of significa…

AdultInjury controlNitrazepammedicine.drug_classAccident preventionPoison controlMotor ActivityToxicologybehavioral disciplines and activitiesHypnoticGrip strengthReaction TimemedicineHumansIngestionNitrazepamPharmacologyPsychomotor learningClinical Trials as Topicbusiness.industryMotor SkillsAnesthesiaDrug EvaluationFemaleSleepbusinessMuscle Contractionmedicine.drugActa Pharmacologica et Toxicologica
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[Use of flunitrazepam for sedation in digestive endoscopy. Our experience].

1988

Use of flunitrazepam for sedation in digestive endoscopy. Our experience

AdultMaleAdolescentPremedicationEndoscopyFlunitrazepamAnxietyMiddle AgedSettore MED/18 - Chirurgia GeneraleanxioliticsSurveys and QuestionnairesGastroscopyHumansFemaleSettore MED/25 - PsichiatriaAgedMinerva chirurgica
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Differences in the topographical distribution of EEG activity during surgical anaesthesia and on emergence from volatile anesthetics.

1994

Computerized processing of a 16 channel EEG allows mapping and display of cortical electrical activity in a useful mode for intraoperative monitoring. We studied the topographical distribution of EEG-activity displayed as spectral maps comparing inhalational anaesthesia with isoflurane or enflurane during surgical anaesthesia and emergence. Two groups of nine patients each were anaesthetized with one of the two regimens. The EEG patterns during steady state end-tidal concentrations of isoflurane (0.7-1.1%) or enflurane (0.8-1.3%) showed highest activity in the frontal and occipital areas. At near awakening the frontal and occipital dominance of delta activity disappeared in both groups and …

AdultMalePremedicationNitrous OxideMedicine (miscellaneous)FlunitrazepamElectroencephalographyCritical Care and Intensive Care MedicineBrain mappingEnfluraneCortex (anatomy)Monitoring IntraoperativemedicineHumansThiopentalAgedBrain Mappingmedicine.diagnostic_testIsofluranebusiness.industryOxazepamVolatile anestheticEnfluraneElectroencephalographySignal Processing Computer-AssistedMiddle Agedmedicine.anatomical_structureIsofluraneAnesthesiaAnesthetics InhalationFemaleTopographical distributionbusinessAnesthesia InhalationInhalational anesthesiamedicine.drugInternational journal of clinical monitoring and computing
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Investigation into mechanisms mediating the inhibitory effect of 1,4-benzodiazepines on mast cells by gene expression profiling.

2013

Abstract Aims This study aims to identify by a molecular genetic approach potential targets in mast cells at which 1,4-benzodiazepines may cause their inhibitory effect on mast cell activity. Main methods Gene expression analyses with microarray gene chip and/or quantitative PCR were performed using 1,4-benzodiazepine-treated human mast cell leukemia HMC-1.2 cells, promyelocytic leukemia HL-60 cells and human mast cells from healthy volunteers and patients with mast cell activation disease (MCAD). Pathway analysis was applied to search for enriched biological functions and canonical pathways within differentially regulated genes. Key findings Both neoplastic and normal human mast cells expr…

AdultMalegenetics [Mastocytosis]Gene ExpressionHL-60 CellsFlunitrazepamBiologyPolymerase Chain ReactionGeneral Biochemistry Genetics and Molecular BiologyClonazepamLYNddc:570medicineTranslocator proteinpharmacology [Flunitrazepam]HumansMast CellsGeneral Pharmacology Toxicology and Pharmaceuticsmethods [Polymerase Chain Reaction]Interleukin 5AgedRegulation of gene expressionBenzodiazepinonesGene Expression Profilingdrug effects [Gene Expression]General MedicineMiddle AgedMast cell leukemiamedicine.diseaseMast cellMicroarray Analysis4'-chlorodiazepamCell biologyInterleukin 33Gene expression profilingmedicine.anatomical_structuremethods [Microarray Analysis]biology.proteinpharmacology [Clonazepam]drug effects [Mast Cells]Femalepharmacology [Benzodiazepinones]Mastocytosismethods [Gene Expression Profiling]
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Binding of flunitrazepam to differentiating neurons cultured in a chemically defined, hormone-supplemented medium

1990

[3H]Flunitrazepam (FNZ) binding to cortical neurons from fetal rat brain was investigated in vitro. The use of a synthetic medium specific for neurons made it possible to plot a developmental curve of3H-FNZ binding in an almost pure neuronal culture. Detectable specific binding was present in vitro at time 0 (that is, the 16th gestational day). A progressive increase of binding, due to an increment in the number of recognition sites, was observed on the subsequent days. The affinity of the specific binding sites to3H-FNZ was enhanced by the addition of exogenous GABA, whereas the density was not affected. © 1990 Plenum Publishing Corporation.

Central nervous systemFlunitrazepamBiologySettore BIO/19 - Microbiologia GeneraleBiochemistrygamma-Aminobutyric acidGABACellular and Molecular NeurosciencemedicineAnimalsBinding siteCells Culturedgamma-Aminobutyric AcidNeuronsFetusCell DifferentiationGeneral MedicineHormonesIn vitroCulture MediaCell biologymedicine.anatomical_structureneuronal cultureCell cultureCerebral cortexSettore MED/26 - NeurologiaFlunitrazepamNeurosciencemedicine.drugNeurochemical Research
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Influence of pH on the benzodiazepine-human serum albumin complex. Circular dichroism studies.

1974

The influence of pH on the binding of benzodiazepine derivatives to HSA was studied by circular dichroism measurements and by gel filtration. The binding of nearly all benzodiazepines is increased by rising the pH from 6.60 to 8.20. For flurazepam, clonazepam, and nitrazepam this increase in binding is due to an increase of the affinities, while for the other substances the affinity remains constant and the number of binding sites is increased from one to two. The changes in binding of the benzodiazepines by rising the pH are explained by a cationic amino acid residue near or at the benzodiazepine binding site of the HSA molecule. This second binding site is not detectable by circular dichr…

Circular dichroismNitrazepamChemical Phenomenamedicine.drug_classStereochemistryFlurazepamSize-exclusion chromatographyPlasma protein bindingFlurazepammedicineHumansBinding siteNitrazepamSerum AlbuminPharmacologyBenzodiazepineBenzodiazepinonesBinding SitesDiazepamChemistryOxazepamCircular DichroismOsmolar ConcentrationChlordiazepoxideGeneral MedicineBenzazepinesHydrogen-Ion ConcentrationHuman serum albuminChemistryKineticsBiophysicsmedicine.drugProtein BindingNaunyn-Schmiedeberg's archives of pharmacology
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gamma-Aminobutyric acid type A/benzodiazepine receptors regulate rat retina neurosteroidogenesis.

1995

Abstract It has been previously shown that retinal ganglion cells have the ability to synthesize steroids including neuroactive steroids such as pregnenolone sulfate. Since ganglion cells possess GABAA/benzodiazepine (BZ) receptors and neurosteroids modulate retinal GABAA receptor function, we investigated the role of these receptors in isolated rat retina neurosteroidogenesis. Ligands for central-type BZ receptors stimulated retinal pregnenolone synthesis. Clonazepam was the most potent ligand examined acting at nanomolar concentrations. Moreover, the effective steroidogenesis stimulatory dose (ED50) for these ligands and theKi to inhibit [3-H]flunitrazepam binding showed a coefficient of …

Malemedicine.medical_specialtyNeuroactive steroidFlunitrazepamBiologyPharmacologyIn Vitro TechniquesRetinal ganglionSynaptic TransmissionRetinaGABAA-rho receptorchemistry.chemical_compoundInternal medicinemedicineAnimalsGABA-A Receptor AgonistsGABA-A Receptor AntagonistsRats WistarMolecular BiologyNeurotransmitter AgentsGABAA receptorGeneral NeuroscienceBicucullineIsoquinolinesReceptors GABA-ARatsKineticsEndocrinologychemistryMuscimolPregnenolonePregnenoloneSteroidsNeurology (clinical)Pregnenolone sulfateNeurogliaDevelopmental Biologymedicine.drugBrain research
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Effects of clozapine metabolites and chronic clozapine treatment on rat brain GABAA receptors

1996

Abstract Similarly to clozapine, a clozapine metabolite, N -desmethylclozapine, but not clozapine N -oxide, antagonized brain γ-aminobutyric acid type A (GABA A ) receptors at high micromolar concentrations. However, daily subcutaneous injections of clozapine (10 and 25 mg/kg) and haloperidol (0.5 mg/kg) for 14 days failed to alter the modulation by GABA of rat cerebrocortical and cerebellar benzodiazepine ([ 3 H]flunitrazepam) or convulsant ( t -[ 35 S]bicyclophosphorothionate) binding sites of the GABA A receptor. The results thus suggest that the GABA A receptor antagonism exerted by chronic in vivo clozapine treatment is weak as compared to this treatment's actions on certain monoamine …

Malemedicine.medical_specialtyTime Factorsmedicine.drug_classDrug Evaluation PreclinicalDesmethylclozapineIn Vitro TechniquesPharmacologyBiologyGABA AntagonistsRats Sprague-Dawleychemistry.chemical_compoundInternal medicinemedicineHaloperidolAnimalsGABA-A Receptor AntagonistsReceptorClozapineClozapinePharmacologyBenzodiazepineGABAA receptorBrainRatsLogistic ModelsEndocrinologychemistryConvulsantHaloperidolFlunitrazepamAntipsychotic Agentsmedicine.drugEuropean Journal of Pharmacology
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Betulin binds to gamma-aminobutyric acid receptors and exerts anticonvulsant action in mice.

2007

The lupane type pentacyclic triterpenes: lupeol, betulin, and betulinic acid are widely distributed natural compounds. Recently, pharmaceutical compositions from plant extracts (family Marcgraviaceae) containing betulinic acid, have been patented as anxiolytic remedies. To extend our knowledge of the CNS effects of the triterpenes, we suggest here that the chemically related lupeol, betulin and betulinic acid may interact with the brain neurotransmitter gamma-aminobutyric acid (GABA) receptors in vitro and in vivo. Using radioligand receptor-binding assay, we showed that only betulin bound to the GABA(A)-receptor sites in mice brain in vitro and antagonised the GABA(A)-receptor antagonist b…

Malemedicine.medical_treatmentClinical BiochemistryAntineoplastic AgentsFlunitrazepamPharmacologyBiologyToxicologyBicucullineBiochemistryAminobutyric acidBehavioral Neurosciencechemistry.chemical_compoundMiceReceptors GABAIn vivoSeizuresBetulinic acidmedicineAnimalsBetulinic AcidReceptorGABA ModulatorsPostural BalanceBiological Psychiatrygamma-Aminobutyric AcidLupeolPharmacologyMice Inbred ICRBetulinAnti-Inflammatory Agents Non-SteroidalTriterpenesAnticonvulsantBiochemistrychemistryMuscle TonusAnticonvulsantsPentacyclic TriterpenesPentacyclic TriterpenesPharmacology, biochemistry, and behavior
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Potato (Solanum tuberosum) Juice Exerts an Anticonvulsant Effect in Mice through Binding to GABA Receptors

2008

Naturally occurring benzodiazepines have been identified in regular food such as wheat and potato, but there is still no evidence that potato extracts can affect CNS responses in vivo. Here we found that undiluted potato juice and potato juice diluted with saline 1 : 2 administered 10 min intracisternally ( I. C.) and 30 min per os before bicuculline exerted significant anticonvulsant activity in the bicuculline-induced seizure threshold test in mice. In vitro, potato juice from different harvests at dilution series from 10 % to 0.000001 %, diluted 100,000-fold, displaced 50 % of gamma-aminobutyric acid (GABA) receptor ligand [ (3)H]GABA and diluted 40-fold displaced 50 % of [(3)H]flunitraz…

Malemedicine.medical_treatmentPharmaceutical SciencePharmacologyPharmacognosyBicucullineMass SpectrometryAnalytical ChemistryMiceReceptors GABAIn vivoDrug DiscoverymedicineAnimalsChromatography High Pressure LiquidSolanum tuberosumPharmacologyMice Inbred ICRDiazepamBehavior AnimalSeizure thresholdPlant ExtractsGABAA receptorChemistryAlkaloidfungiOrganic Chemistryfood and beveragesBicucullineAnticonvulsantComplementary and alternative medicineBiochemistryMolecular MedicineAnticonvulsantsFlunitrazepammedicine.drugPlanta Medica
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