Search results for "Azoles"

showing 10 items of 899 documents

Nitric oxide as neuromodulator of sympathetic transmission in rat vas deferens.

1998

Summary Electrical field stimulation (EFS) of muscle strips in vitro elicited a tetrodotoxin (TTX)-sensitive biphasic contractile response consisting of a phasic component followed by a tonic one. The amplitude of both components of the response was impaired by Nω-nitro-L-arginine and potentiated by sodium nitroprusside. Cystamine caused a reduction in amplitude of both phasic and tonic componets of the response to EFS. Neither Nω-nitro-L-arginine, sodium nitroprusside, nor cystamine induced changes in the resting muscle tone, or in the contractile response to exogenous agonists ATP and noradrenaline (NA). The nitric oxide scavenger, 2-phenyl-4,4,5,5-tetramethylimidazoline-1-oxyl-3-oxide, i…

MaleNitroprussidemedicine.medical_specialtySympathetic Nervous SystemCystamineNeurotransmissionNitric OxideNitroarginineTonic (physiology)Nitric oxideCyclic N-Oxideschemistry.chemical_compoundVas DeferensCystamineInternal medicinemedicineExtracellularAnimalsEnzyme InhibitorsRats WistarPharmacologyGeneral NeuroscienceVas deferensImidazolesElectric StimulationRatsmedicine.anatomical_structureEndocrinologychemistryGuanylate CyclaseTetrodotoxinSodium nitroprussideNitric Oxide Synthasemedicine.drugMuscle ContractionJournal of autonomic pharmacology
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Liver subcellular fractions from rats treated by organosulfur compounds from Allium modulate mutagen activation

2000

The effects of in vivo administration of naturally occurring organosulfur compounds (OSCs) from Allium species were studied on the activation of several mutagens. Male SPF Wistar rats were given p.o. one of either diallyl sulfide (DAS), diallyl disulfide (DADS), dipropyl sulfide (DPS) or dipropyl disulfide (DPDS) during 4 consecutive days and the ability of hepatic S9 and microsomes from treated rats to activate benzo[a]pyrene (BaP), cyclophosphamide (CP), dimethylnitrosamine (DMN), N-nitrosopiperidine (N-PiP) and 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP) was determined in the Ames test. Administration of DAS, DPS and DPDS resulted in a significant increase of the activation of…

MaleNitrosaminesHealth Toxicology and Mutagenesis[SDV]Life Sciences [q-bio]MutagenSulfidesmedicine.disease_causeIsozymeAlliumDimethylnitrosamineAmes testPropane03 medical and health scienceschemistry.chemical_compound0302 clinical medicineCytochrome P-450 Enzyme SystemBenzo(a)pyreneCytochrome P-450 CYP1A1GeneticsmedicineAnimalsDisulfidesRats WistarCyclophosphamideComputingMilieux_MISCELLANEOUS030304 developmental biology0303 health sciencesDose-Response Relationship DrugMutagenicity TestsDiallyl disulfideImidazolesCytochrome P-450 CYP2E1CYP2E1RatsAllyl Compounds[SDV] Life Sciences [q-bio]Dose–response relationshipBiochemistrychemistry030220 oncology & carcinogenesisCytochrome P-450 CYP2B1ToxicityMicrosomes LiverMicrosomeLiver ExtractsOxidoreductasesMutagensSubcellular Fractions
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Translational read-through of the RP2 Arg120stop mutation in patient iPSC-derived retinal pigment epithelium cells.

2014

Mutations in the RP2 gene lead to a severe form of X-linked retinitis pigmentosa. RP2 patients frequently present with nonsense mutations and no treatments are currently available to restore RP2 function. In this study, we reprogrammed fibroblasts from an RP2 patient carrying the nonsense mutation c.519C>T (p.R120X) into induced pluripotent stem cells (iPSC), and differentiated these cells into retinal pigment epithelial cells (RPE) to study the mechanisms of disease and test potential therapies. RP2 protein was undetectable in the RP2 R120X patient cells, suggesting a disease mechanism caused by complete lack of RP2 protein. The RP2 patient fibroblasts and iPSC-derived RPE cells showed phe…

MaleNonsense mutationInduced Pluripotent Stem CellsGene ExpressionRetinal Pigment EpitheliumBiologymedicine.disease_causeBioinformaticschemistry.chemical_compoundYoung AdultGTP-Binding ProteinsRetinitis pigmentosaGeneticsmedicineHumansCiliaFibroblastInduced pluripotent stem cellEye ProteinsMolecular BiologyGenetics (clinical)MutationOxadiazolesRetinal pigment epitheliumIntracellular Signaling Peptides and ProteinsMembrane ProteinsRetinalCell DifferentiationEpithelial CellsGeneral MedicineArticlesFibroblastsmedicine.diseaseCellular Reprogramming3. Good healthAtalurenCell biologyProtein Transportmedicine.anatomical_structurePhenotypechemistryProtein BiosynthesisMutationHuman molecular genetics
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A randomized phase II study of ganetespib, a heat shock protein 90 inhibitor, in combination with docetaxel in second-line therapy of advanced non-sm…

2015

Background: This trial was designed to evaluate the activity and safety of ganetespib in combination with docetaxel in advanced non-small cell lung cancer (NSCLC) and to identify patient populations most likely to benefit from the combination. Patients and methods: Patients with one prior systemic therapy for advanced disease were eligible. Docetaxel (75 mg/m<sup>2</sup> on day 1) was administered alone or with ganetespib (150 mg/m<sup>2</sup> on days 1 and 15) every 3 weeks. The primary end points were progression-free survival (PFS) in two subgroups of the adenocarcinoma population: patients with elevated lactate dehydrogenase (eLDH) and mutated KRAS (mKRAS). Resul…

MaleOncologyHSP90 inhibitormedicine.medical_specialtyLung NeoplasmsPopulationGanetespibPhases of clinical researchDocetaxelAdenocarcinomaNeutropeniaDisease-Free SurvivalProto-Oncogene Proteins p21(ras)Carcinoma Non-Small-Cell LungInternal medicineAntineoplastic Combined Chemotherapy ProtocolsmedicineHumansHSP90 Heat-Shock ProteinsLung cancereducationAgedProportional Hazards Modelseducation.field_of_studyL-Lactate Dehydrogenasebusiness.industryHazard ratioHematologyMiddle AgedTriazolesmedicine.diseaseTreatment OutcomeAdvanced NSCLCOncologyDocetaxelGanetespibAdenocarcinomaFemaleTaxoidsbusinessmedicine.drugAnnals of Oncology
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Osteonecrosis of the Jaw in Patients With Metastatic Renal Cell Cancer Treated With Bisphosphonates and Targeted Agents: Results of an Italian Multic…

2015

Osteonecrosis of the jaw (ONJ) associated with the use of bisphosphonates has been rarely reported in metastatic renal cell cancer (RCC) patients. Since the introduction of combined therapies consisting of nitrogen-containing bisphosphonates (NBPs) and targeted agents, an increasing number of RCC patients were reported to develop ONJ, suggesting that therapeutic angiogenesis suppression might increase the risk of ONJ in NBPs users. We performed a multicenter retrospective study and reviewed literature data to assess the occurrence and to investigate the nature of ONJ in RCC patients taking NBPs and targeted agents. Nine Italian Centers contributed to the data collection. Patients with expos…

MaleOncologyIndolesAngiogenesis InhibitorsPyrroleBevacizumab; m-TOR inhibitor; Sorafenib; Sunitinib; Zoledronic acidRetrospective StudieAntineoplastic Combined Chemotherapy ProtocolsSunitinibAged 80 and overDiphosphonatesSunitinibImidazolesOsteonecrosisKidney NeoplasmMiddle AgedSorafenibKidney NeoplasmsBevacizumabDiphosphonateItalyOncologyOsteonecrosiFemaleAngiogenesis InhibitorHumanmedicine.drugSorafenibmedicine.medical_specialtyBevacizumab; m-TOR inhibitor; Sorafenib; Sunitinib; Zoledronic acid; Aged; Aged 80 and over; Angiogenesis Inhibitors; Antineoplastic Combined Chemotherapy Protocols; Carcinoma Renal Cell; Diphosphonates; Female; Humans; Imidazoles; Indoles; Italy; Jaw; Kidney Neoplasms; Male; Middle Aged; Osteonecrosis; Pyrroles; Retrospective Studies; Oncology; UrologyBevacizumabUrologyInternal medicinemedicineHumansPyrrolesIn patientMetastatic renal cell cancerImidazoleCarcinoma Renal CellZoledronic acidAgedRetrospective StudiesAntineoplastic Combined Chemotherapy Protocolbusiness.industryRetrospective cohort studymedicine.diseasem-TOR inhibitorSurgeryZoledronic acidJawIndolebusinessOsteonecrosis of the jaw
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Osteonecrosis of the jaw (ONJ) in renal cell cancer patients after treatment including zoledronic acid or denosumab.

2014

Dear Editor, The paper by Henry et al. published by Supportive Care in Cancer comparing efficacy of denosumab versus zoledronic acid in patients with bone metastases of advanced solid tumours [1] comes to integrate the original reports of three pivotal large randomized phase 3 trials [2–4], the publication by Saad et al. about osteonecrosis of the jaw (ONJ) in those three trials [5], and the combined outcome analysis by Lipton et al. [6]. Henry et al. [1] reported outcomes of the single trial conducted on patients with solid tumours (except breast or prostate cancers, object of other two trials) [2, 3], excluding patients with multiple myeloma: This ad hoc analysis confirmed the superiority…

MaleOncologymedicine.medical_specialtyBevacizumabONJ renal cell cancerBone NeoplasmsAntibodies Monoclonal HumanizedPazopanibSettore MED/28 - Malattie OdontostomatologicheNeoplasmsInternal medicinemedicineHumansBone ResorptionEverolimusBone Density Conservation AgentsDiphosphonatesSunitinibbusiness.industryImidazolesmedicine.diseaseTemsirolimusZoledronic acidDenosumabOncologyFemalebusinessOsteonecrosis of the jawmedicine.drug
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Bone marrow characteristics predict outcome in a multicenter cohort of primary immune thrombocytopenia patients treated with thrombopoietin analogs

2019

It is well established that immune thrombocytopenia (ITP) results from increased immune mediated platelet destruction (anti-platelets antibodies, autoreactive T cells, and reduction of regulatory T cells) along with impaired production in the bone marrow.1 The latter has been attributed to both cellular and humoral mediators that cause suppression of megakaryocyte production and maturation.2 Current standard first line therapy consists of corticosteroids, with or without intravenous Ig, achieving about 70-80% response rate. However, a consistent proportion of patients would relapse after corticosteroid discontinuation or tapering, and requires further therapy. ...

MaleOncologymedicine.medical_specialtyRecombinant Fusion ProteinsEltrombopagBone Marrow CellsImmune Thrombocytopenic PurpuraReceptors FcBenzoateschemistry.chemical_compoundInternal medicinemedicineHumansOnline Only ArticlesThrombopoietinRetrospective StudiesPurpura Thrombocytopenic IdiopathicRomiplostimbusiness.industryRetrospective cohort studyromiplostimHematologyMiddle AgedImmune thrombocytopeniaClinical trialHydrazinesmedicine.anatomical_structureThrombopoietinchemistryCohortPyrazolesFemaleBone marroweltrombopagbusinessFollow-Up Studiesmedicine.drugHaematologica
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Disseminated tuberculosis in a patient treated with a JAK2 selective inhibitor: a case report

2012

Abstract Background Primary myelofibrosis is a myeloproliferative disorder characterized by bone marrow fibrosis, abnormal cytokine expression, splenomegaly and anemia. The activation of JAK2 and the increased levels of circulating proinflammatory cytokines seem to play an important role in the pathogenesis of myelofibrosis. Novel therapeutic agents targeting JAKs have been developed for the treatment of myeloproliferative disorders. Ruxolitinib (INCB018424) is the most recent among them. Case presentation To our knowledge, there is no evidence from clinical trials of an increased risk of tuberculosis during treatment with JAK inhibitors. Here we describe the first case of tuberculosis in a…

MaleOncologymedicine.medical_specialtyRuxolitinibTuberculosisSettore MED/17 - Malattie InfettiveAnemiaAntitubercular AgentsMyelofibrosislcsh:MedicineCase ReportGeneral Biochemistry Genetics and Molecular BiologyProinflammatory cytokineMyeloproliferative DisordersInternal medicineNitrilesmedicineHumansTuberculosisMyelofibrosislcsh:Science (General)lcsh:QH301-705.5Medicine(all)Janus kinase 2biologyLatent tuberculosisBiochemistry Genetics and Molecular Biology(all)business.industryTuberculosis Myelofibrosis Ruxolitiniblcsh:RGeneral MedicineJanus Kinase 2medicine.diseasePyrimidinesRuxolitiniblcsh:Biology (General)Primary MyelofibrosisImmunologybiology.proteinPyrazolesbusinessmedicine.druglcsh:Q1-390BMC Research Notes
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A novel cyclo-oxygenase-2 inhibitor modulates catabolic and antiinflammatory mediators in osteoarthritis.

2004

ITB (6-(p-bromophenyl)amino-7-(p-chlorophenyl)indazolo[2',3':1,5]-1,2,4-triazolo[4,3-a]-1,3,5-benzotriazepine) is a novel inhibitor of cyclo-oxygenase-2 (COX-2) with antiinflammatory activity in animal models. In the present study, we investigated the effect of this compound on the production of catabolic or antiinflammatory mediators in osteoarthritis (OA) cartilage. In OA cartilage explants, ITB inhibited the production of prostaglandin E(2) (PGE(2)), tumour necrosis factor-alpha (TNF-alpha) and matrix metalloproteinase-13 (MMP-13) in a concentration-dependent manner, whereas nitrite was partially reduced. On the contrary, ITB increased the production of interleukin (IL)-10 and the expres…

MaleOxygenaseIndazolesmedicine.medical_treatmentAnti-Inflammatory AgentsOsteoarthritisPharmacologyBiochemistryOsteoarthritismedicineHumansCyclooxygenase InhibitorsProstaglandin E2AgedPharmacologyCyclooxygenase 2 InhibitorsChemistryCatabolismCartilageAnti-Inflammatory Agents Non-SteroidalInterleukinMembrane ProteinsAzepinesTriazolesmedicine.diseaseIsoenzymesInterleukin 10Cytokinemedicine.anatomical_structureCartilageBiochemistryCyclooxygenase 2Prostaglandin-Endoperoxide SynthasesFemalemedicine.drugBiochemical pharmacology
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Modulatory effects of nitric oxide-active drugs on the anticonvulsant activity of lamotrigine in an experimental model of partial complex epilepsy in…

2007

Abstract Background The effects induced by administering the anticonvulsant lamotrigine, the preferential inhibitor of neuronal nitric oxide synthase 7-nitroindazole and the precursor of NO synthesis L-arginine, alone or in combination, on an experimental model of partial complex seizures (maximal dentate gyrus activation) were studied in urethane anaesthetized rats. The epileptic activity of the dentate gyrus was obtained through the repetitive stimulation of the angular bundle and maximal dentate gyrus activation latency, duration and post-stimulus afterdischarge duration were evaluated. Results Either Lamotrigine (10 mg kg-1) or 7-nitroindazole (75 mg kg-1) i.p. administration had an ant…

MalePARTIAL COMPLEX EPILEPSYIndazolesArgininemedicine.medical_treatmentLamotriginePharmacologyArginineLamotrigineNitric OxideSettore BIO/09 - Fisiologialcsh:RC321-571Nitric oxideCellular and Molecular Neurosciencechemistry.chemical_compoundEpilepsy Complex PartialmedicineAnimalsDrug InteractionsEnzyme InhibitorsRats Wistarlcsh:Neurosciences. Biological psychiatry. NeuropsychiatryNitric oxide Lamotrigine epilepsy controlbiologyTriazinesExperimental modelGeneral NeuroscienceDentate gyruslcsh:QP351-495BrainElectric StimulationRatsNitric oxide synthaseDisease Models Animallcsh:Neurophysiology and neuropsychologyAnticonvulsantnervous systemchemistryDentate Gyrusbiology.proteinAnticonvulsantsNitric Oxide SynthaseResearch Articlemedicine.drugBMC Neuroscience
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