Search results for "Phene"

showing 10 items of 863 documents

In vitro anti-inflammatory effects of AZD8999, a novel bifunctional muscarinic acetylcholine receptor antagonist /β2-adrenoceptor agonist (MABA) comp…

2019

Recent evidence indicates that AZD8999 (LAS190792), a novel muscarinic acetylcholine receptor antagonist and β2-adrenoceptor agonist (MABA) in development for chronic respiratory diseases, induces potent and sustained relaxant effects in human bronchi by adressing both muscarinic acetylcholine receptors and β2-adrenoceptor. However, the anti-inflammatory effects of the AZD8999 monotherapy or in combination with corticosteroids are unknown. This study investigates the anti-inflammatory effects of AZD8999 in monotherapy and combined with fluticasone propionate in neutrophils from healthy and chronic obstructive pulmonary disease (COPD) patients. Peripheral blood neutrophils from healthy and C…

MalePulmonologyNeutrophilsPhysiologyAnti-Inflammatory AgentsPharmacologyPathology and Laboratory MedicineBiochemistryPulmonary Disease Chronic ObstructiveWhite Blood CellsGlucocorticoid receptorAnimal CellsMuscarinic acetylcholine receptorMedicine and Health SciencesPost-Translational ModificationPhosphorylationReceptorImmune ResponseMultidisciplinaryPharmaceuticsQRDrug SynergismMiddle AgedReceptors MuscarinicHealthy VolunteersBody FluidsChemistryBloodPhysical SciencesQuinolinesMedicineDrug Therapy CombinationFemalemedicine.symptomCellular TypesAnatomymedicine.drugResearch ArticleSignal TransductionAgonistTransmembrane Receptorsmedicine.drug_classp38 mitogen-activated protein kinasesChronic Obstructive Pulmonary DiseaseImmune CellsScienceImmunologyInflammationMuscarinic AntagonistsThiophenesFluticasone propionateSigns and SymptomsDrug TherapyCyclohexanesDiagnostic MedicinemedicineHumansAdrenergic beta-2 Receptor AgonistsAgedInflammationBlood CellsDose-Response Relationship Drugbusiness.industryAntagonistChemical CompoundsBiology and Life SciencesProteinsCell BiologyAcetylcholine ReceptorsFluticasoneMuscarinic Acetylcholine ReceptorsReceptors Adrenergic beta-2PropionatesbusinessReceptor Antagonist TherapyPLoS ONE
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Histamine and serotonin released from the rat perfused heart by compound 48/80 or by allergen challenge influence noradrenaline or acetylcholine exoc…

1994

Terminal nerve fibres of the autonomic nervous system closely approach mast cells in peripheral organs, and mutual influences between release of neurotransmitters or mast cell mediators may cause neuro-immunological interactions. We have studied the influence of mast cell degranulation on the release of endogenous noradrenaline and newly incorporated acetylcholine (such as 14C-choline/acetylcholine overflow) evoked by stimulation of extrinsic postganglionic sympathetic or preganglionic vagal nerves in the rat Langendorff heart perfused with Tyrode solution. Compound 48/80 perfused in normal hearts, or ovalbumin infused into hearts from rats sensitized to ovalbumin, enhanced the overflow of …

MaleSerotoninmedicine.medical_specialtyLangendorff heartSerotonergicHistamine ReleaseExocytosisNorepinephrinechemistry.chemical_compoundInternal medicinemedicineAnimalsp-Methoxy-N-methylphenethylaminePharmacology (medical)Mast CellsRats WistarNeurotransmitterPharmacologyThioperamideChemistryMyocardiumAllergensCompound 48/80AcetylcholineRatsPerfusionEndocrinologyHistamine H3 receptorAcetylcholineHistaminemedicine.drugFundamental & Clinical Pharmacology
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Characterization of 5-hydroxytryptamine release from isolated rabbit and rat trachea: the role of neuroendocrine epithelial cells and mast cells

1995

Rabbit or rat isolated tracheae were incubated in vitro, and the release of 5-hydroxytryptamine (5-HT) and its metabolite 5-hydroxyindoleacetic acid (5-HIAA) was determined by HPLC with electrochemical detection. Release of 5-HT from rabbit tracheae could be evoked by the calcium ionophore A 23187 and, in a calcium-dependent manner, by depolarizing concentrations of potassium (45 mmol/l), but not by the mast cell degranulating drug compound 48/80. High potassium- and A 23187-evoked release of 5-HT was markedly higher from tracheae of newborn compared to adult rabbits. In rabbit tracheae, mechanical removal of the mucosa resulted in 80-90% reduction in tissue 5-HT and in a similar reduction …

MaleSerotoninmedicine.medical_specialtychemistry.chemical_elementIn Vitro TechniquesCalciumCalcium in biology5-HydroxytryptophanRats Sprague-DawleyPhentolamineInternal medicinemedicinePrazosinAnimalsp-Methoxy-N-methylphenethylamineSecretionMast CellsCalcimycinPharmacologyChemistryDepolarizationGeneral MedicineReceptors Adrenergic alphaMast cellNeurosecretory SystemsIn vitroRatsTracheamedicine.anatomical_structureEndocrinologyFemaleRabbitsmedicine.drugNaunyn-Schmiedeberg's Archives of Pharmacology
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The effects of transdermal rotigotine on non-motor symptoms of Parkinson's disease: a multicentre, observational, retrospective, post-marketing study

2017

This study evaluated the effect of ≥6 months of transdermal rotigotine on non-motor and motor symptoms of patients with advanced Parkinson's disease.The study was conducted in Spain between September 2011 and December 2012 (ClinicalTrials.gov: NCT01504529). The primary efficacy variable was the change from baseline in non-motor symptoms, as assessed by changes in Parkinson's Disease Non-Motor Symptoms Questionnaire total scores at 6 months. Secondary endpoints included the assessment of motor symptoms by Unified Parkinson's Disease Rating Scale III scores.Data from 378 patients (mean age: 70.2 years; 56.9% male) with Parkinson's disease receiving rotigotine from were collected. Mean disease…

MaleSleep Wake Disordersmedicine.medical_specialtyParkinson's diseaseTetrahydronaphthalenesThiophenesDiseaseAdministration CutaneousMotor symptoms03 medical and health sciences0302 clinical medicineSurveys and QuestionnairesProduct Surveillance PostmarketingmedicineHumans030212 general & internal medicineAgedRetrospective StudiesTransdermalAged 80 and overbusiness.industryGeneral NeuroscienceParkinson DiseaseRotigotineGeneral MedicineUrination Disordersmedicine.diseaseClinical PracticeTreatment OutcomeSpainDopamine AgonistsPhysical therapyNon motorFemaleObservational studyCognition Disordersbusiness030217 neurology & neurosurgerymedicine.drugInternational Journal of Neuroscience
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Ambulatory monitoring of systolic hypertension in the elderly: Eprosartan/hydrochlorothiazide compared with losartan/hydrochlorothiazide (INSIST tria…

2010

Introduction: Systolic hypertension is very common in the elderly and is strongly associated with the risk of cardiovascular and cerebrovascular events. The control of systolic hypertension is difficult and most patients require combination antihypertensive therapy. Few data are available regarding the efficacy of angiotensin II receptor antagonists on systolic hypertension of the elderly. The aim of this double-blind, double-dummy, randomized, parallel-group, multicenter study was to assess the efficacy of eprosartan 600 mg in combination with hydrochlorothiazide (HCTZ)12.5 mg in comparison with losartan 50 mg in combination with HCTZ 12.5 mg, in reducing blood pressure in elderly patients…

MaleSystolic hypertensionOffice VisitsPharmacologySeverity of Illness Indexlaw.inventionHydrochlorothiazideRandomized controlled triallawAngiotensin II Type 1 Receptor BlockerPharmacology (medical)DiureticsImidazolesGeneral MedicineBlood Pressure Monitoring AmbulatoryAntihypertensive AgentLosartanHydrochlorothiazideTreatment OutcomeAcrylatesHypertensionCardiologyDrug Therapy CombinationFemaleDrug MonitoringHumanmedicine.drugmedicine.medical_specialtyAmbulatory blood pressureSystoleLosartan/hydrochlorothiazideThiopheneselderly patientselderlyLosartanStatistics NonparametricDouble-Blind MethodThiopheneInternal medicinemedicineDiureticHumansImidazoleAntihypertensive AgentsAgedAnalysis of Variancebusiness.industryeprosartanEprosartanmedicine.diseaseambulatory blood pressure monitoringAcrylateBlood pressureOffice VisitbusinessAngiotensin II Type 1 Receptor BlockersAdvances in therapy
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Pretreatment with prasugrel in non-ST-segment elevation acute coronary syndromes

2013

Item does not contain fulltext BACKGROUND: Although P2Y12 antagonists are effective in patients with non-ST-segment elevation (NSTE) acute coronary syndromes, the effect of the timing of administration--before or after coronary angiography--is not known. We evaluated the effect of administering the P2Y12 antagonist prasugrel at the time of diagnosis versus administering it after the coronary angiography if percutaneous coronary intervention (PCI) was indicated. METHODS: We enrolled 4033 patients with NSTE acute coronary syndromes and a positive troponin level who were scheduled to undergo coronary angiography within 2 to 48 hours after randomization. Patients were randomly assigned to recei…

Malemedicine.medical_specialtyAcute coronary syndromePrasugrelmedicine.medical_treatmentPremedicationMyocardial InfarctionHemorrhageThiophenesCoronary AngiographyPiperazinesPercutaneous Coronary InterventionDouble-Blind MethodInternal medicinemedicineHumansMyocardial infarctionAcute Coronary SyndromeCoronary Artery BypassAgedCardiovascular diseases [NCEBP 14]business.industryMedicine (all)Hazard ratioAcute Coronary Syndrome; Aged; Coronary Artery Bypass; Double-Blind Method; Female; Hemorrhage; Humans; Male; Middle Aged; Myocardial Infarction; Percutaneous Coronary Intervention; Piperazines; Prasugrel Hydrochloride; Purinergic P2Y Receptor Antagonists; Thiophenes; Coronary Angiography; Premedication; Medicine (all)Percutaneous coronary interventionGeneral MedicineThrombolysisMiddle Agedta3121medicine.diseaseConventional PCICardiologyPurinergic P2Y Receptor AntagonistsFemalebusinessPrasugrel HydrochlorideTIMImedicine.drug
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Impact of comorbidities on pharmacotherapy of painful diabetic neuropathy in clinical practice.

2014

Abstract Aims We evaluated the impact of baseline comorbidities on the effectiveness of duloxetine and anticonvulsants (pregabalin/gabapentin) in patients with painful diabetic neuropathy in clinical care. Methods Outcomes from a 6-month, observational study with 2575 patients initiating/switching DPNP treatment were analyzed post-hoc. Propensity scoring was used to adjust for baseline factors influencing treatment choice in 1523 patients receiving duloxetine or anticonvulsants. Analysis of covariance models with fixed effects for baseline pain, treatment, propensity score, baseline characteristics or comorbidities, and their interaction with treatment were used to estimate LSmean effects o…

Malemedicine.medical_specialtyGabapentinCyclohexanecarboxylic AcidsEndocrinology Diabetes and MetabolismPregabalinPregabalinComorbidityThiophenesDuloxetine Hydrochloridechemistry.chemical_compoundEndocrinologyDiabetic NeuropathiesInternal MedicinemedicineDuloxetineHumansPain ManagementBrief Pain InventoryAminesDepression (differential diagnoses)gamma-Aminobutyric AcidAgedPain MeasurementRetrospective StudiesAnalgesicsbusiness.industryChronic painMiddle Agedmedicine.diseasePrognosisTreatment OutcomechemistryJoint painPropensity score matchingPhysical therapyAnticonvulsantsFemalemedicine.symptomGabapentinbusinessmedicine.drugJournal of diabetes and its complications
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Dopamine acting through D2 receptors modulates the expression of PSA-NCAM, a molecule related to neuronal structural plasticity, in the medial prefro…

2008

A "neuroplastic" hypothesis proposes that changes in neuronal structural plasticity may underlie the aetiology of depression and the action of antidepressants. The medial prefrontal cortex (mPFC) is affected by this disorder and shows an intense expression of the polysialylated form of the neural cell adhesion molecule (PSA-NCAM), a plasticity-associated molecule, which is expressed mainly in interneurons. The monoamines serotonin, dopamine and noradrenaline are the principal targets of antidepressant action. Pharmacological manipulation of serotonin levels regulates synaptophysin and PSA-NCAM expression in the adult mPFC. However, the involvement of structural plasticity on the antidepress…

Malemedicine.medical_specialtyInterneuronDopamineSynaptophysinPrefrontal CortexNeural Cell Adhesion Molecule L1Synaptic TransmissionDopamine agonistRats Sprague-DawleyDevelopmental NeuroscienceDopamineDopamine receptor D2Internal medicinePhenethylaminesmedicineAnimalsNeuronsAnalysis of VarianceMicroscopy ConfocalNeuronal PlasticityGlutamate DecarboxylaseReceptors Dopamine D2ChemistryDopaminergicDopamine antagonistImmunohistochemistryRatsmedicine.anatomical_structureEndocrinologynervous systemNeurologyDopamine receptorDopamine AgonistsSialic AcidsDopamine AntagonistsHaloperidolNeural cell adhesion moleculeNeurosciencemedicine.drugExperimental Neurology
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Contributions of ACE and mast cell chymase to endogenous angiotensin II generation and leucocyte recruitment in vivo

2011

Aims In vitro studies suggest that mast cell chymase (MCP) is more important than angiotensin-converting enzyme (ACE) for generating angiotensin II (Ang II) within the cardiovascular system. We investigated in vivo the relative contributions of ACE and MCP to leucocyte recruitment induced by endogenously generated Ang II. Methods and results Exposure of the murine cremasteric microcirculation of C57BL/6 mice to Ang I (100 nM for 4 h) induced leucocyte–endothelium interactions. Either losartan (an Ang II receptor-1 antagonist, AT1) or enalapril (an ACE inhibitor), but not chymostatin (a chymase inhibitor), inhibited Ang I-induced responses. Mast cell degranulation with compound 48/80 (CMP48/…

Malemedicine.medical_specialtyPhysiologymedicine.drug_classReceptor expressionPeptidyl-Dipeptidase AReceptor Angiotensin Type 1MiceChymasesCell MovementPhysiology (medical)Internal medicineLeukocytesmedicineAnimalsp-Methoxy-N-methylphenethylamineMast CellsMast cell stabilizerEnalaprilAngiotensin II receptor type 1ChemistryAngiotensin IIChymaseAngiotensin IIMice Inbred C57BLEndocrinologyLosartanACE inhibitorcardiovascular systemAngiotensin ICardiology and Cardiovascular Medicinehormones hormone substitutes and hormone antagonistsmedicine.drugCardiovascular Research
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Clinic modelling randomised trials (CMRT's) in animals as a new intermediate between biological experiments and randomised clinical trials: applicati…

1998

Malemedicine.medical_specialtySwinemedicine.medical_treatmentPremedicationImmunologyPharmacology toxicologyRanitidineHistamine ReleaseDouble-Blind MethodMedicineAnimalsDimethindenep-Methoxy-N-methylphenethylamineAnesthesiaCluster randomised controlled trialIntensive care medicineIntraoperative ComplicationsRandomized Controlled Trials as TopicPharmacologybusiness.industryClinical trialDisease Models AnimalHistamine H2 AntagonistsSurgical Procedures OperativeHistamine H1 AntagonistsSwine MiniatureAntihistamineFemalebusinessCimetidineInflammation research : official journal of the European Histamine Research Society ... [et al.]
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