Search results for "Azine"

showing 10 items of 1589 documents

Endothelium- and nitric oxide-dependent vasorelaxing activities of gamma-butyrobetaine esters: possible link to the antiischemic activities of mildro…

2004

Mildronate [3-(2,2,2-trimethylhydrazine) propionate (THP)] is an antiischemic drug acting mainly via inhibition of fatty acid beta-oxidation. Some effects of the drug cannot be explained by the latter mechanism. We tested the eventual nitric oxide (NO) dependence of the mildronate action. Mildronate, gamma-butyrobetaine (GBB) and GBB methyl ester induced transient increases in nitric oxide (NO) concentrations in rat blood and myocardium. In vitro, these compounds neither modified the activities of purified neuronal and endothelial recombinant nitric oxide synthases (NOSs) nor were able to interact with their active site. GBB induced vasodilatation at high concentrations only (EC50 = 5 x 10(…

MaleEndotheliumNitric Oxide Synthase Type IIIStereochemistryDrug Evaluation PreclinicalMyocardial IschemiaVasodilationAorta ThoracicNitric OxideMuscle Smooth VascularNitric oxidechemistry.chemical_compoundCarnitinemedicineAnimalsEndotheliumRats WistarPharmacologychemistry.chemical_classificationbiologyElectron Spin Resonance SpectroscopyActive siteFatty acidDrug SynergismRatsNitric oxide synthaseBetaineVasodilationDrug Combinationsmedicine.anatomical_structureEnzymeNG-Nitroarginine Methyl Esterchemistrybiology.proteinPropionateNitric Oxide SynthaseDitiocarbMethylhydrazinesEuropean journal of pharmacology
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In vivo genotoxicity of selected herbicides in the mouse bone-marrow micronucleus test

1997

The herbicides alachlor, atrazine, terbuthylazine, gluphosinate-ammonium, isoproturon, pendimethaline and trifluralin were tested for genotoxicity in the mouse bone-marrow micronucleus test (MNT). Both atrazine and trifluraline caused a significant increase in the number of micronuclei at doses of 1,400 mg/kg body weight in female mice only. Alachlor, terbuthylazine, gluphosinate-ammonium, isoproturon and pendimethaline did not have any genotoxic effect in the mouse bone-marrow micronucleus test in either female or male animals.

MaleHealth Toxicology and Mutagenesis010501 environmental sciencesPharmacologyToxicologymedicine.disease_cause01 natural sciencesToxicologyMice03 medical and health scienceschemistry.chemical_compoundBone MarrowIn vivomedicineAnimalsAtrazine030304 developmental biology0105 earth and related environmental sciences0303 health sciencesMicronucleus TestsHerbicidesAlachlorTrifluralinGeneral MedicineTerbuthylazinechemistryToxicityMicronucleus testFemaleGenotoxicityMutagensArchives of Toxicology
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A Simple Microassay for the Determination of Hydrazine in Biological Samples. Effect of Hydrazine and Isoniazid on Liver and Brain Glutathione

1987

A simple microassay for the determination of hydrazine in laboratory samples is presented. The colored product of the reaction of p-dimethylaminobenzaldehyde with hydrazine was tested at 470 nm using double-beam mode in different samples. Internal standards and data on blood serum, liver, and brain of rats treated with hydrazine or isoniazid are presented. The tissue glutathione content of these rats was determined, and the possible implication of glutathione in the brain toxicity of hydrazine is discussed.

MaleHealth Toxicology and MutagenesisMetaboliteToxicologyAnalytical Chemistrychemistry.chemical_compoundBlood serumSpectrophotometryIsoniazidmedicineAnimalsEnvironmental ChemistryHydrazine (antidepressant)Brain ChemistryChemical Health and SafetyChromatographymedicine.diagnostic_testIsoniazidMetabolismGlutathioneGlutathioneRatsHydrazinesLiverchemistryBiochemistryToxicitymedicine.drugJournal of Analytical Toxicology
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Genotoxic effects of the herbicides alachlor, atrazine, pendimethaline, and simazine in mammalian cells

1994

MaleHealth Toxicology and MutagenesisSimazineSimazineToxicologyRats Sprague-Dawleychemistry.chemical_compoundAcetamidesAnimalsHumansEcotoxicologyLymphocytesAtrazineCells CulturedAniline CompoundsHerbicidesMutagenicity TestsChemistrybusiness.industryAlachlorGeneral MedicinePesticidePollutionRatsBiotechnologyLiverAtrazinebusinessSister Chromatid ExchangeDNA DamageBulletin of Environmental Contamination and Toxicology
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Transmission of HIV Drug Resistance and the Predicted Effect on Current First-line Regimens in Europe

2016

Transmitted human immunodeficiency virus drug resistance in Europe is stable at around 8%. The impact of baseline mutation patterns on susceptibility to antiretroviral drugs should be addressed using clinical guidelines. The impact on baseline susceptibility is largest for nonnucleoside reverse transcriptase inhibitors.

MaleHuman immunodeficiency virus 1EtravirineRNA directed DNA polymerase inhibitordarunavirHIV InfectionsSettore MED/42 - Igiene Generale E Applicata:Disciplines and Occupations::Health Occupations::Medicine::Public Health [Medical Subject Headings]:Organisms::Eukaryota::Animals::Chordata::Vertebrates::Mammals::Primates::Haplorhini::Catarrhini::Hominidae::Humans [Medical Subject Headings]Salud públicageneticsInhibidores de proteasas:Analytical Diagnostic and Therapeutic Techniques and Equipment::Investigative Techniques::Epidemiologic Methods::Data Collection::Vital Statistics::Morbidity::Prevalence [Medical Subject Headings]atazanavirmedia_commontransmission:Geographicals::Geographic Locations::Europe [Medical Subject Headings]3. Good healthmicrobial sensitivity testpriority journalEurope ; HIV-1 ; antiretroviral therapy ; drug resistance ; transmissionHIV/AIDSlamivudineReverse Transcriptase Inhibitors/pharmacologyanti human immunodeficiency virus agentDrugMicrobiology (medical)medicine.medical_specialtyantiviral susceptibility:Phenomena and Processes::Genetic Phenomena::Genetic Variation::Mutation [Medical Subject Headings]media_common.quotation_subjectantiretroviral therapy030106 microbiologyHIV Infections/drug therapy:Chemicals and Drugs::Chemical Actions and Uses::Pharmacologic Actions::Therapeutic Uses::Anti-Infective Agents::Antiviral Agents::Anti-Retroviral Agents::Reverse Transcriptase Inhibitors [Medical Subject Headings]Microbial Sensitivity TestsRILPIVIRINEArticleEFAVIRENZ03 medical and health sciencestransmitted drug resistanceSDG 3 - Good Health and Well-beingHumansTransmissionhuman:Phenomena and Processes::Physiological Phenomena::Pharmacological Phenomena::Drug Resistance [Medical Subject Headings]REVERSE-TRANSCRIPTASE INHIBITORSRilpivirinaINTEGRASEMUTATIONSabacavirmajor clinical studyVirologyInfecciones por VIHRegimenAntiretroviral therapy; Drug resistance; Europe; HIV-1; Transmission; Medicine (all); Microbiology (medical); Infectious DiseaseschemistryDrug resistance:Chemicals and Drugs::Heterocyclic Compounds::Heterocyclic Compounds 1-Ring::Oxazines::Benzoxazines [Medical Subject Headings]MutationHIV-10301 basic medicinenevirapineDrug resistanceCommunicable diseases:Analytical Diagnostic and Therapeutic Techniques and Equipment::Investigative Techniques::Epidemiologic Methods::Statistics as Topic::Confidence Intervals [Medical Subject Headings]chemistry.chemical_compoundantiviral therapyINFECTIONMedicine and Health SciencesPrevalence:Analytical Diagnostic and Therapeutic Techniques and Equipment::Investigative Techniques::Epidemiologic Methods::Data Collection::Surveys and Questionnaires [Medical Subject Headings]ViralNon-U.S. Gov'tReverse-transcriptase inhibitorantiretrovirus agentResearch Support Non-U.S. Gov'tMedicine (all)Human immunodeficiency virus infected patientMiddle AgedvirologyPREVALENCEAntiretroviral therapyEncuestas y CuestionariosANTIRETROVIRAL TREATMENTEuropeInfectious DiseasesHIV-1/drug effectsHIV Protease Inhibitors/pharmacologyRilpivirineReverse Transcriptase Inhibitors:Diseases::Immune System Diseases::Immunologic Deficiency Syndromes::HIV Infections [Medical Subject Headings]FemaleHIV drug resistancemedicine.drugAdultHuman immunodeficiency virus proteinase inhibitor:Chemicals and Drugs::Organic Chemicals::Nitriles::Rilpivirine [Medical Subject Headings]EfavirenzAnti-HIV AgentsResearch SupportResistencia a medicamentosSettore MED/17 - MALATTIE INFETTIVEantiviral resistanceInternal medicineAnti-HIV Agents/pharmacologyDrug Resistance ViralJournal Articlemedicine:Chemicals and Drugs::Chemical Actions and Uses::Pharmacologic Actions::Molecular Mechanisms of Pharmacological Action::Enzyme Inhibitors::Protease Inhibitors [Medical Subject Headings]abacavir plus lamivudineEuropa (Continente)Antiretroviral therapy; Drug resistance; Europe; HIV-1; Transmission; Adult; Anti-HIV Agents; Drug Resistance Viral; Europe; Female; HIV Infections; HIV Protease Inhibitors; HIV-1; Humans; Male; Microbial Sensitivity Tests; Middle Aged; Mutation; Prevalence; Reverse Transcriptase Inhibitors; Microbiology (medical); Infectious DiseasesemtricitabinenonhumanIntervalos de confianzadrug resistanceMutaciónAntiretroviral therapy; Drug resistance; Europe; HIV-1; Transmissionbusiness.industryHIVpredictionInhibidores de la transcriptasa inversaHIV Protease InhibitorsHuman immunodeficiency virus 1 infectiontenofovirINDIVIDUALSDrug Resistance Viral/geneticsBenzoxazinasETRAVIRINEdrug effects3121 General medicine internal medicine and other clinical medicinePrevalenciabusiness
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Double Drug Delivery Using Capped Mesoporous Silica Microparticles for the Effective Treatment of Inflammatory Bowel Disease

2019

[EN] Silica mesoporous microparticles loaded with both rhodamine B fluorophore (S1) or hydrocortisone (S2), and capped with an olsalazine derivative, are prepared and fully characterized. Suspensions of Si and S2 in water at an acidic and a neutral pH show negligible dye/drug release, yet a notable delivery took place when the reducing agent sodium dithionite is added because of hydrolysis of an azo bond in the capping ensemble. Additionally, olsalazine fragmentation induced 5-aminosalicylic acid (5-ASA) release. In vitro digestion models show that S1 and S2 solids are suitable systems to specifically release a pharmaceutical agent in the colon. In vivo pharmacokinetic studies in rats show …

MaleHydrocortisoneTECNOLOGIA DE ALIMENTOSReducing agentPharmaceutical Science02 engineering and technologyMesoporous silica microparticles030226 pharmacology & pharmacyInflammatory bowel diseaseSodium dithionite03 medical and health scienceschemistry.chemical_compoundHydrolysisDrug Delivery Systems0302 clinical medicineQUIMICA ORGANICAIn vivoDrug DiscoveryQUIMICA ANALITICAmedicineRhodamine BAnimalsGated materialsRats WistarMesalamineOlsalazineRhodaminesColon targeted releaseQUIMICA INORGANICAMesoporous silicaColitisInflammatory Bowel DiseasesSilicon Dioxide021001 nanoscience & nanotechnologySmart drug delivery materialsRatschemistryDrug deliveryMolecular Medicine0210 nano-technologymedicine.drugNuclear chemistry
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A Polymorphism in the Crhr1 Gene Determines Stress Vulnerability in Male Mice

2014

Chronic stress is a risk factor for psychiatric disorders but does not necessarily lead to uniform long-term effects on mental health, suggesting modulating factors such as genetic predispositions. Here we address the question whether natural genetic variations in the mouse CRH receptor 1 (Crhr1) locus modulate the effects of adolescent chronic social stress (ACSS) on long-term stress hormone dysregulation in outbred CD1 mice, which allows a better understanding of the currently reported genes × environment interactions of early trauma and CRHR1 in humans. We identified 2 main haplotype variants in the mouse Crhr1 locus that modulate the long-term effects of ACSS on basal hypothalamic-pitui…

MaleHypothalamo-Hypophyseal SystemGenotypeGene ExpressionPituitary-Adrenal SystemLocus (genetics)Single-nucleotide polymorphismRegulatory Sequences Nucleic AcidBiologyBinding CompetitivePolymorphism Single NucleotideReceptors Corticotropin-Releasing HormoneMiceEndocrinologyGene FrequencyGenetic predispositionAnimalsHumansGenetic Predisposition to DiseaseChronic stressCRHR1 GeneGeneIn Situ HybridizationSocial stressGeneticsBehavior AnimalTriazinesHaplotypeHaplotypesPituitary GlandPyrazolesFemaleGene-Environment InteractionCorticosteroneStress PsychologicalSignal TransductionEndocrinology
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Increased levels of Th17 cells are associated with non-neuronal acetylcholine in COPD patients.

2014

T-lymphocytes, including Th17-cells and T-cells expressing acetylcholine (ACh), are key components of systemic inflammation in chronic obstructive pulmonary disease (COPD). We investigated whether ACh promotes Th17 cells in COPD. ACh, IL-17A, IL-22, RORγt, FOXP3 expression and AChIL-17A, AChIL-22, AChRORγt coexpression was evaluated in peripheral blood mononuclear cells (PBMC) from COPD patients (n=16), healthy smokers (HS) (n=12) and healthy control subjects (HC) (n=13) (cultured for 48 h with PMA) by flow cytometry. Furthermore, we studied the effect of Tiotropium (Spiriva®) (100 nM) and Olodaterol (1nM) alone or in combination, and of hemicholinium-3 (50 μM) on AChIL-17A, AChIL-22, AChRO…

MaleImmunologyIntracellular SpaceScopolamine DerivativesPharmacologySystemic inflammationPeripheral blood mononuclear cellCholinergic AntagonistsFlow cytometrychemistry.chemical_compoundPulmonary Disease Chronic ObstructiveRAR-related orphan receptor gammaRisk FactorsmedicineImmunology and AllergyHumansTiotropium BromideAgedAged 80 and overCOPDmedicine.diagnostic_testbusiness.industryInterleukinsOlodaterolInterleukin-17FOXP3Forkhead Transcription FactorsHematologyMiddle AgedNuclear Receptor Subfamily 1 Group F Member 3medicine.diseaseAcetylcholineBenzoxazineschemistryLeukocytes MononuclearTh17 CellsFemalemedicine.symptombusinessAcetylcholinemedicine.drugImmunobiology
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Modulation of high impulsivity and attentional performance in rats by selective direct and indirect dopaminergic and noradrenergic receptor agonists

2011

Rationale Impulsivity is associated with a number of psychiatric disorders, most notably attention deficit/hyperactivity disorder (ADHD). Drugs that augment catecholamine function (e.g. methylphenidate and the selective noradrenaline reuptake inhibitor atomoxetine) have clinical efficacy in ADHD, but their precise mechanism of action is unclear. Objective The objective of this study is to investigate the relative contribution of dopamine (DA) and noradrenaline (NA) to the therapeutic effects of clinically effective drugs in ADHD using rats selected for high impulsivity on the five-choice serial reaction time task (5CSRTT). Methods We examined the effects of direct and indirect DA and NA rec…

MaleImpulsivityQuinpiroleDopamineSerial LearningAtomoxetine HydrochlorideImpulsivityChoice BehaviorPiperazines03 medical and health sciences0302 clinical medicineQuinpiroleDopaminemental disordersAnimals Outbred StrainsReaction TimemedicineAnimalsAttentionOriginal InvestigationPharmacologyPropylaminesMethylphenidateDopaminergicAtomoxetineGBR-12909Adrenergic AgonistsGuanfacineRats030227 psychiatry3. Good healthGuanfacineSumaniroleFive-choice serial reaction time taskAtomoxetine; Dopamine; Five-choice serial reaction time task; GBR-12909; Guanfacine; Impulsivity; Methylphenidate; Noradrenaline; Quinpirole; Sumanirole; Adrenergic Agonists; Animals; Animals Outbred Strains; Atomoxetine Hydrochloride; Attention; Benzimidazoles; Choice Behavior; Dopamine Agonists; Guanfacine; Impulsive Behavior; Male; Methylphenidate; Piperazines; Propylamines; Quinpirole; Rats; Reaction Time; Serial Learning; PharmacologyAnesthesiaDopamine AgonistsImpulsive BehaviorNoradrenalineAtomoxetineMethylphenidateBenzimidazolesmedicine.symptomPsychologyNeuroscience030217 neurology & neurosurgerymedicine.drugAtomoxetine hydrochloride
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Randomized Trial of Brinzolamide/Brimonidine Versus Brinzolamide Plus Brimonidine for Open-Angle Glaucoma or Ocular Hypertension

2014

Introduction Fixed-combination intraocular pressure (IOP)—lowering medications simplify treatment regimens for patients requiring 2 ocular hypotensive agents to maintain sufficiently low IOP. The aim of this study was to evaluate the safety and efficacy of fixed-combination brinzolamide 1%/brimonidine 0.2% (BBFC) versus concomitant administration of brinzolamide 1% plus brimonidine 0.2% (BRINZ + BRIM) in patients with open-angle glaucoma or ocular hypertension. Methods This was a prospective, phase 3, multicenter, double-masked, 6-month trial. Patients who had insufficient IOP control with monotherapy or who were receiving 2 IOP-lowering medications were randomized 1:1 to receive twice-dail…

MaleIntraocular pressuremedicine.medical_specialtyConcomitantgenetic structuresIntraocular pressureBrinzolamideThiazinesOcular hypertensionGlaucomaOcular hypertensionlaw.inventionTonometry OcularRandomized controlled trialDouble-Blind MethodlawOphthalmologyQuinoxalinesConcomitant TherapyMedicineHumansPharmacology (medical)Fixed combinationCarbonic anhydrase inhibitorAntihypertensive AgentsOriginal ResearchAgedMedicine(all)Sulfonamidesbusiness.industryBrimonidineAlpha-2 agonistSimbrinza®GlaucomaGeneral MedicineMiddle Agedmedicine.diseaseeye diseasesDysgeusiaOphthalmologyDrug CombinationsTreatment OutcomeBrimonidine TartrateFemalesense organsmedicine.symptombusinessGlaucoma Open-Anglemedicine.drugAdvances in Therapy
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