Search results for "Piperazines"

showing 10 items of 135 documents

Five-Year Follow-up of Patients Receiving Imatinib for Chronic Myeloid Leukemia

2006

The cause of chronic myeloid leukemia (CML) is a constitutively active BCR-ABL tyrosine kinase. Imatinib inhibits this kinase, and in a short-term study was superior to interferon alfa plus cytarabine for newly diagnosed CML in the chronic phase. For 5 years, we followed patients with CML who received imatinib as initial therapy.We randomly assigned 553 patients to receive imatinib and 553 to receive interferon alfa plus cytarabine and then evaluated them for overall and event-free survival; progression to accelerated-phase CML or blast crisis; hematologic, cytogenetic, and molecular responses; and adverse events.The median follow-up was 60 months. Kaplan-Meier estimates of cumulative best …

MaleOncologymedicine.medical_specialtyFusion Proteins bcr-ablAntineoplastic AgentsKaplan-Meier EstimateChronic phase chronic myelogenous leukemiaDisease-Free SurvivalPiperazineschemistry.chemical_compoundLeukemia Myelogenous Chronic BCR-ABL Positivehemic and lymphatic diseasesInternal medicineAntineoplastic Combined Chemotherapy ProtocolsOmacetaxine mepesuccinatemedicineHumansneoplasmsbusiness.industryPonatinibCytarabineInterferon-alphaMyeloid leukemiaImatinibGeneral MedicineProtein-Tyrosine KinasesSurvival AnalysisSurvival RateDasatinibPyrimidinesTreatment OutcomeImatinib mesylatechemistryNilotinibBenzamidesImmunologyImatinib MesylateFemalebusinessFollow-Up Studiesmedicine.drugNew England Journal of Medicine
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Phenytoin-induced glutathione depletion in rat peripheral nerve

1995

Abstract Administration of high doses (150–250 mg/kg body weight) of phenytoin (DPH) promote a 40% decrease in glutathione (GSH) content of rat sciatic nerve. This DPH-induced GSH depletion is accompanied with an electrophysiological impairment of peripheral neuromuscular function. H7 (20 mg/kg body weight IP, 30 min prior to DPH), a protein kinase C inhibitor, was able to prevent the DPH-induced GSH depletion only at the lower DPH dose used. This same inhibitor completely prevented the electrophysiological impairment at the lower DPH dose, and only partially at the higher DPH dose used. These results confirm the hypothesis of a DPH-dependent activation of PKC (that might be triggered by, o…

MalePhenytoinAntioxidantmedicine.medical_treatmentAction PotentialsIn Vitro TechniquesPharmacologymedicine.disease_causeBiochemistryPiperazineschemistry.chemical_compound1-(5-Isoquinolinesulfonyl)-2-MethylpiperazinePhysiology (medical)polycyclic compoundsmedicineAnimalsEnzyme InhibitorsRats WistarMuscle SkeletalEvoked PotentialsProtein Kinase CProtein kinase CMotor NeuronsAnalysis of Variancetechnology industry and agricultureNeurotoxicityGlutathioneIsoquinolinesmedicine.diseaseGlutathioneSciatic NerveRatsKineticschemistryBiochemistryPhenytoinAnticonvulsantslipids (amino acids peptides and proteins)Sciatic nerveOxidative stressIntracellularmedicine.drugFree Radical Biology and Medicine
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Clinical presentation and treatment of gastrointestinal stromal tumors.

2006

Aims and background Gastrointestinal stromal tumors (GISTs), although rare, are the most common mesenchymal neoplasms affecting the gastrointestinal tract. We present our experience in the treatment of localized and metastatic disease and a review of literature. Patients and methods Nine patients were observed from April 2002 to July 2004. Eight tumors were in the gastric area and J was in the small bowel. In 5 cases, complete surgical removal was performed, and none of these patients underwent adjuvant therapy. The remaining 4 cases, with locally advanced or recurrent disease, were treated with imatinib. Results The patients with localized disease treated only by surgery did not relapse. I…

MaleReoperationCancer Researchmedicine.medical_specialtyGastrointestinal Stromal TumorsAntineoplastic AgentsDiseaseGastroenterologyPiperazines03 medical and health sciences0302 clinical medicineInternal medicinemedicineAdjuvant therapyHumansRadical surgeryProtein Kinase InhibitorsAgedGastrointestinal tractbusiness.industryStandard treatmentImatinibGeneral MedicineMiddle AgedSurvival AnalysisSurgeryPyrimidinesTreatment OutcomeImatinib mesylategastrointestinal stromal tumors treatment.OncologyChemotherapy Adjuvant030220 oncology & carcinogenesisLocalized diseaseBenzamidesImatinib MesylateFemale030211 gastroenterology & hepatologybusinessmedicine.drug
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Carboxyamidotriazole-Orotate Inhibits the Growth of Imatinib-Resistant Chronic Myeloid Leukaemia Cells and Modulates Exosomes-Stimulated Angiogenesis

2012

The Bcr/Abl kinase has been targeted for the treatment of chronic myelogenous leukaemia (CML) by imatinib mesylate. While imatinib has been extremely effective for chronic phase CML, blast crisis CML are often resistant. New therapeutic options are therefore needed for this fatal disease. Although more common in solid tumors, increased microvessel density was also reported in chronic myelogenous leukaemia and was associated with a significant increase of angiogenic factors, suggesting that vascularity in hematologic malignancies is a controlled process and may play a role in the leukaemogenic process thus representing an alternative therapeutic target. Carboxyamidotriazole-orotate (CTO) is …

MaleResearch ValidityPhysiologyAngiogenesisTumor PhysiologyFusion Proteins bcr-ablCancer Treatmentlcsh:MedicinePharmacologyExosomesCardiovascular PhysiologyBiochemistryPiperazinesHematologic Cancers and Related DisordersMicechemistry.chemical_compoundCell Movementhemic and lymphatic diseasesMolecular Cell BiologyBasic Cancer ResearchMedicine and Health SciencesPhosphorylationPost-Translational ModificationExtracellular Signal-Regulated MAP Kinaseslcsh:ScienceChronic Myelogenous LeukemiaMultidisciplinaryABLNeovascularization PathologicGene Expression Regulation LeukemicChemistryHematologyResearch AssessmentOncologyBenzamidesImatinib MesylateMedicineOncology AgentsAntiangiogenesis Therapymedicine.drugResearch ArticleChronic Myeloid LeukemiaAntineoplastic AgentsResearch and Analysis MethodsCell GrowthCell Line TumorLeukemia Myelogenous Chronic BCR-ABL PositiveLeukemiasCell AdhesionHuman Umbilical Vein Endothelial CellsmedicineAnimalsHumansRNA MessengerPhosphotyrosineBiologyCell ProliferationOrotic AcidTumor microenvironmentCarboxyamidotriazoleInterleukin-8lcsh:RBiology and Life SciencesProteinsCancers and NeoplasmsImatinibTriazolesmedicine.diseaseXenograft Model Antitumor AssaysRetractionExosomePyrimidinesImatinib mesylateDrug Resistance NeoplasmCarboxyamidotriazole Orotatelcsh:QAngiogenesisCell Adhesion MoleculesProto-Oncogene Proteins c-aktDevelopmental BiologyChronic myelogenous leukemiaPLoS ONE
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Effectiveness of dolutegravir-based regimens as either first-line or switch antiretroviral therapy: data from the Icona cohort

2019

Introduction: Concerns about dolutegravir (DTG) tolerability in the real-life setting have recently arisen. We aimed to estimate the risk of treatment discontinuation and virological failure of DTG-based regimens from a large cohort of HIV-infected individuals. Methods: We performed a multicentre, observational study including all antiretroviral therapy (ART)-naïve and virologically suppressed treatment-experienced (TE) patients from the Icona (Italian Cohort Naïve Antiretrovirals) cohort who started, for the first time, a DTG-based regimen from January 2015 to December 2017. We estimated the cumulative risk of DTG discontinuation regardless of the reason and for toxicity, and of virologica…

Maleadverse eventadverse events; antiretroviral therapy; cohort study; discontinuation; dolutegravir; toxicity; Adult; Anti-HIV Agents; Cohort Studies; Dideoxynucleosides; Female; HIV Infections; Heterocyclic Compounds 3-Ring; Humans; Italy; Male; Middle Aged; Prospective Studies; Retrospective Studies; Tenofovir; Treatment Outcomeadverse events; antiretroviral therapy; cohort study; discontinuation; dolutegravir; toxicity;HIV InfectionsPiperazinesCohort Studies0302 clinical medicineHeterocyclic CompoundsAbacavirRetrospective StudieMedicineHIV InfectionProspective Studies030212 general & internal medicineProspective cohort studyResearch Articlesadverse events; antiretroviral therapy; cohort study; discontinuation; dolutegravir; toxicityHazard ratioMiddle AgedDideoxynucleosidedolutegravirTreatment OutcomeInfectious DiseasesTolerabilityItalyCohortFemalePublic Health0305 other medical scienceHeterocyclic Compounds 3-RingResearch Articlemedicine.drugHumanAdultmedicine.medical_specialtyAnti-HIV AgentsPyridonesantiretroviral therapySettore MED/17 - MALATTIE INFETTIVE3-RingLower riskNO03 medical and health sciencesInternal medicineOxazinescohort studyHumansTenofovirRetrospective Studies030505 public healthbusiness.industryEnvironmental and Occupational HealthPublic Health Environmental and Occupational HealthAnti-HIV AgenttoxicityRetrospective cohort studyantiretroviral therapy; dolutegravir; cohort study; discontinuation; toxicity; adverse eventsDideoxynucleosidesadverse eventsDiscontinuationProspective Studieadverse events; antiretroviral therapy; cohort study; discontinuation; dolutegravir; toxicity; Public Health Environmental and Occupational Health; Infectious DiseasesCohort Studiebusinessdiscontinuation
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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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Role of K+ and Ca2+ fluxes in the cerebroarterial vasoactive effects of sildenafil

2007

The aim of this study was to assess the role of K(+) and Ca(2+) fluxes in the cerebroarterial vasoactive effects of the phosphodiesterase-5 inhibitor sildenafil. We used isolated rabbit basilar arteries to assess the effects of extracellular K(+) raising on sildenafil-induced vasodilatation, and studied the pharmacological interaction of sildenafil with selective modulators of membrane K(+) and Ca(2+) channels. Expression of Kv1 subunits of K(+) channels was assessed at messenger and protein levels. Parallel experiments were carried out with zaprinast for comparison. Sildenafil (10 nM-0.1 mM) induced concentration-dependent relaxation of endothelin-1 (10 nM)-precontracted arteries, which wa…

Malemedicine.medical_specialtyCalcium Channels L-Typemedicine.drug_mechanism_of_actionPhosphodiesterase InhibitorsVasodilationIn Vitro TechniquesPharmacologyPiperazinesSildenafil Citratechemistry.chemical_compoundInternal medicinemedicineAnimalsChannel blockerRNA MessengerSulfonesPharmacologyTetraethylammoniumDose-Response Relationship DrugChemistryDepolarization3-Pyridinecarboxylic acid 14-dihydro-26-dimethyl-5-nitro-4-(2-(trifluoromethyl)phenyl)- Methyl esterIberiotoxinEndocrinologyPurinesBasilar ArterycGMP-specific phosphodiesterase type 5PotassiumShaker Superfamily of Potassium ChannelsCalciumRabbitsZaprinastPhosphodiesterase 5 inhibitorEuropean Journal of Pharmacology
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Gastrointestinal stromal tumour of the rectum: Report of a case and review of literature

2008

Gastrointestinal stromal tumour (GIST) is a rare tumour of the gastrointestinal tract which does not generally originate in the rectum. The authors describe a case of a 70-year-old man who underwent an anterior resection of the rectum for a low-risk GIST. The patient was not given adjuvant chemotherapy with imatinib and is still disease-free 30 mo after surgery. The authors conclude that although rectal GIST is extremely uncommon, it should be included in differential diagnosis when a tumour in the rectum is detected. Biopsy of the tumour is essential, since this makes it possible to reach a sure preoperative diagnosis based on the immunohistological features of the CD117 and CD34. Although…

Malemedicine.medical_specialtyGastrointestinal Stromal TumorsCD34RectumAntigens CD34Antineoplastic AgentsCase ReportPiperazinesGIST;BiopsymedicineHumansneoplasmsAgedGastrointestinal tractGiSTmedicine.diagnostic_testbiologyRectal NeoplasmsCD117business.industryGastroenterologyGeneral MedicineCombined Modality Therapydigestive system diseasesSurgeryProto-Oncogene Proteins c-kitPyrimidinesTreatment Outcomemedicine.anatomical_structureImatinib mesylateBenzamidesImatinib Mesylatebiology.proteinDifferential diagnosisbusinessGISTWorld Journal of Gastroenterology
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Lower self-reported depression in patients with erectile dysfunction after treatment with sildenafil

2001

Abstract Background: Depressive symptoms in men with erectile dysfunction (ED) may improve under successful ED treatment. Self-reported depressive symptoms were compared in men with ED after sildenafil treatment to a group of untreated patients. Methods: In an open study, self-reported depressive symptoms of 54 men after successful treatment with sildenafil (>4 weeks) and 51 men awaiting ED treatment were investigated with the Center of Epidemiologic Studies–Depression Scale (CES–D). CES–D items were subjected to an exploratory factor analysis and group differences in CES–D items and factors were analyzed. Results: Groups were comparable with respect to demographic characteristics and illne…

Malemedicine.medical_specialtyPersonality InventoryDepression scaleSildenafilmedia_common.quotation_subjectPiperazinesSildenafil Citratechemistry.chemical_compoundErectile DysfunctionInternal medicinemedicineHumansIn patientSulfonesRisk factorDepression (differential diagnoses)Agedmedia_commonSelection biasDepressionMiddle Agedmedicine.diseasePsychiatry and Mental healthClinical PsychologyCross-Sectional StudiesTreatment OutcomeErectile dysfunctionchemistryPurinesPsychologyAfter treatmentClinical psychologyJournal of Affective Disorders
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Relaxant effect of sildenafil in the rabbit basilar artery

2005

We hypothesized that sildenafil, inhibitor of phosphodiesterase-5 (PDE-5), interacts with the nitric oxide (NO)-cGMP pathway in the cerebral arteries and shows vasoactive effects. To prove it in the isolated rabbit basilar artery, we compared the effects of sildenafil with other PDE-5 inhibitors, assessed the endothelial dependence of the vasoactive responses, and used modulators of the cGMP and cAMP signaling processes. Sildenafil (10 nM-0.1 mM) induced concentration-dependent relaxations of endothelin-1 (10 nM)-precontracted basilar artery, which were partially inhibited both in endothelium-denuded arteries and in arteries precontracted by depolarization with KCl (50 mM). Endothelin-1 (1 …

Malemedicine.medical_specialtyPhosphodiesterase InhibitorsPhysiologySildenafilVasodilator AgentsCerebral arteriesVasodilationIn Vitro TechniquesPiperazinesSildenafil Citratechemistry.chemical_compound3'5'-Cyclic-GMP PhosphodiesterasesQuinoxalinesmedicine.arteryInternal medicinemedicineBasilar arteryAnimalsSulfonesCyclic Nucleotide Phosphodiesterases Type 5PharmacologyOxadiazolesDose-Response Relationship DrugPhosphoric Diester HydrolasesPDE5 drug designVasodilationNG-Nitroarginine Methyl EsterEndocrinologychemistryGuanylate CyclasePurinesBasilar Arterycardiovascular systemMolecular MedicineRabbitsSodium nitroprussideNitric Oxide SynthaseSoluble guanylyl cyclaseZaprinastSignal Transductionmedicine.drugVascular Pharmacology
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