Search results for "Piper"

showing 10 items of 632 documents

Akute interstitielle Nephritis nach Piperacillin

1989

A 75-year-old woman developed fever, exanthema and nonoliguric renal failure 16 days after the beginning of Piperacillin treatment. Renal biopsy revealed lympho-plasmacellular acute interstitial nephritis (AIN). A lymphocyte-transformation-test showed significant stimulation of patient's lymphocytes by Piperacillin. Corticosteroid-therapy correlated to clinical and renal improvement. Nevertheless the patient died of foudroyant septicemia caused by E. coli. Our report describes the first immunologically documented case of AIN following Piperacillin treatment.

medicine.medical_specialtyAcute interstitial nephritismedicine.diagnostic_testbusiness.industryGeneral MedicineGastroenterologyMolecular medicineLymphocyte transformationInternal medicineDrug DiscoveryImmunologymedicineMolecular MedicineRenal biopsybusinessGenetics (clinical)Piperacillinmedicine.drugKlinische Wochenschrift
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Blocking Jak/STAT signalling using tofacitinib inhibits angiogenesis in experimental arthritis

2021

Abstract Objective During rheumatoid arthritis (RA), the angiogenic processes, occurring with pannus-formation, may be a therapeutic target. JAK/STAT-pathway may play a role and the aim of this work was to investigate the inhibiting role of a JAK-inhibitor, tofacitinib, on the angiogenic mechanisms occurring during RA. Methods After ethical approval, JAK-1, JAK-3, STAT-1, STAT-3 and VEGF expression was evaluated on RA-synovial-tissues. In vitro, endothelial cells (ECs), stimulated with 20 ng/ml of VEGF and/or 1 μM of tofacitinib, were assessed for tube formation, migration and proliferation, by Matrigel, Boyden chamber assay and ki67 gene-expression. In vivo, 32 mice received collagen (coll…

medicine.medical_specialtyAngiogenesisArthritisDiseases of the musculoskeletal systemPharmacologyPyrroleMiceRheumatoid arthritis Angiogenesis TofacitinibPiperidinePiperidinesIn vivoInternal medicineMedicineAnimalsHumansPyrrolesRheumatoid arthritisRheumatoid arthritiTube formationMatrigelEndothelial CellTofacitinibbusiness.industryAnimalSynovial MembraneEndothelial Cellsmedicine.diseaseArthritis ExperimentalRheumatologyAngiogenesiPyrimidinesPyrimidineRC925-935TofacitinibRheumatoid arthritisAngiogenesisbusinessHumanResearch Article
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Mucosa-dependent muscarinic liberation of prostaglandins from rat isolated trachea.

1995

1. The present study examined whether cholinoceptor stimulation modulates the release of arachidonic acid-derived mediators from rat isolate tracheae. 2. Tracheae were preincubated with [3H]-arachidonic acid and the outflow of 3H-compounds was determined. Acetylcholine and the muscarinic agonist, carbachol but not nicotine, increased the rate of tritium outflow maximally by about 30%. The M3 receptor-preferring antagonist rho-fluoro-hexahydrosiladiphenidol was more effective than pirenzepine and methoctramine in antagonizing the effect of acetylcholine. 3. High performance liquid chromatography analysis (methanol gradient) of the released 3H-compounds showed that one peak, co-eluting with […

medicine.medical_specialtyCarbacholAcetonitrilesMuscarinic AntagonistsIn Vitro TechniquesMuscarinic AgonistsMuscarinic agonistRats Sprague-Dawleychemistry.chemical_compoundPiperidinesInternal medicineMuscarinic acetylcholine receptormedicineMethoctramineAnimalsDrug InteractionsAcetylcholine receptorPharmacologyArachidonic AcidDose-Response Relationship DrugMuscarinic acetylcholine receptor M1PirenzepineAcetylcholineRatsTracheaEndocrinologychemistryProstaglandinslipids (amino acids peptides and proteins)FemaleAcetylcholinemedicine.drugResearch Article
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Tissue Differences in the Effect of Atropine on the Evoked Release of Acetylcholine

1979

The effect of atropine on the release of acetylcholine (ACh) from different peripheral parasympathetically innervated tissues was investigated. My enteric plexus The longitudinal muscle-myenteric plexus preparation of the guinea-pig was incubated in eserinecontaining Tyrode solution. The ACh release evoked by high K+ (45 or 108 μ) or by the nicotinic drug dimethylphenylpiperazinium (DMPP) (10 pM) was increased by atropine (0.1–10 μ) in a concentration-dependent fashion. Muscarinic agonists (oxotremorine; propargylester of arecaidine) prevented the facilitatory effect of atropine on ACh release. These results suggest that the ACh release from the myenteric plexus is regulated via presynaptic…

medicine.medical_specialtyChemistryDimethylphenylpiperaziniumInhibitory postsynaptic potentialAtropineEndocrinologyNicotinic agonistInternal medicineMuscarinic acetylcholine receptormedicineOxotremorineAcetylcholineMyenteric plexusmedicine.drug
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Different muscarine receptors mediate the prejunctional inhibition of [3H]-noradrenaline release in rat or guinea-pig iris and the contraction of the…

1989

To investigate the muscarine receptor type mediating inhibition of [3H]-noradrenaline release from the isolated rat and guinea-pig iris we have determined the potency of antimuscarinic drugs to antagonize the methacholine-induced inhibition of [3H]-noradrenaline overflow evoked by field stimulation (3 Hz, 2 min). The prejunctional apparent affinities were compared with those obtained for postjunctional muscarine receptors mediating the methacholine-induced contraction of the isolated rabbit iris sphincter muscle. Prejunctional apparent affinity constants of pirenzepine (6.67), himbacine (8.51), methoctramine (7.92), 4-diphenylacetoxy-N-methylpiperidine methiodide (4-DAMP, 8.00), hexahydro-d…

medicine.medical_specialtyContraction (grammar)Iris sphincter muscleIrisIn Vitro TechniquesBiologyGuinea pigNorepinephrinechemistry.chemical_compoundPiperidinesInternal medicineMuscarinic acetylcholine receptormedicineAnimalsMethacholine CompoundsNeurotransmitterReceptorPharmacologyMuscarineMuscle SmoothRats Inbred StrainsGeneral MedicineReceptors MuscarinicElectric StimulationRatsKineticsmedicine.anatomical_structureEndocrinologychemistrySphincterRabbitsMuscle ContractionNaunyn-Schmiedebergs Archives of Pharmacology
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Analysis of Rabbit Vascular Responses to DBI, an Ingol Derivative Isolated from Euphorbia canariensis

1997

Abstract We have analysed the effects of 7,12-O-diacetyl-8-O-benzoil-2,3-diepiingol (DBI), an ingol derivative isolated from E. canariensis, on isometric tension developed by isolated rabbit basilar and carotid arteries. Concentration-response curves to DBI (10−8 - 3 × 10−5 m) were obtained cumulatively in both arteries at resting tension and active tone (KC1, 50 mm). At resting tension, DBI induced a concentration-dependent contraction, which was not inhibited in Ca2+-free medium. H7 (1-(5-isoquinoline sulphonyl)-2-methylpiperazine dichloride) (10−4 m) inhibited the DBI-induced contraction both in basilar and in carotid arteries. Calmidazolium (10−4 m) inhibited the maximum contraction of …

medicine.medical_specialtyContraction (grammar)LatexCarotid Artery CommonMuscle RelaxationPharmaceutical ScienceProstacyclinNitric OxideNitroarginineMuscle Smooth VascularEuphorbia canariensisCalmodulin1-(5-Isoquinolinesulfonyl)-2-MethylpiperazineInternal medicinemedicine.arterymedicineBasilar arteryAnimalsEnzyme InhibitorsProtein Kinase CPharmacologyPlants MedicinalLagomorphabiologyPlant Extractsbiology.organism_classificationEpoprostenolEndocrinologymedicine.anatomical_structureBasilar ArteryCirculatory systemcardiovascular systemCalciumRabbitsDiterpenesMuscle Contractionmedicine.drugBlood vesselArteryJournal of Pharmacy and Pharmacology
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Inhibition of intracellular Ca2+ release by a Rho-kinase inhibitor for the treatment of ischemic damage in primary cultured rat hippocampal neurons.

2008

The effects of hydroxy fasudil, a specific Rho-kinase inhibitor, on behavior and brain neuronal activity in animal studies have been described previously. However, whether a Rho-kinase inhibitor can directly protect neurons against ischemic damage and the molecular mechanisms underlying these effects are poorly understood. The present work was designed to investigate the effect of hydroxy fasudil against oxygen-glucose deprivation (OGD) induced acute neuronal injury and the underlying mechanisms in vitro. Pretreatment with hydroxy fasudil at 5 and 10 microM could concentration-dependently improve cell viability and decrease Lactate dehydrogenase (LDH) level in extracellular solution of neur…

medicine.medical_specialtyExcitotoxicityIntracellular SpaceGlutamic AcidBiologymedicine.disease_causeNeuroprotectionHippocampusCalcium in biologyPotassium ChlorideRats Sprague-DawleyCalcium imagingAdenosine TriphosphateIschemiaInternal medicine1-(5-Isoquinolinesulfonyl)-2-MethylpiperazinemedicineAnimalsHypoxiaProtein Kinase InhibitorsCells CulturedPharmacologyNeuronsrho-Associated KinasesDose-Response Relationship DrugCalcium channelFasudilGlutamate receptorRatsEndocrinologyGlucoseRho kinase inhibitorCalciumEuropean journal of pharmacology
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Diacylglycerol kinase α mediatses 17-β-estradiol-induced proliferation, motility, and anchorage-independent growth of Hec-1A endometrial cancer cell …

2011

Increased levels of endogenous and/or exogenous estrogens are one of the well known risk factors of endometrial cancer. Diacylglycerol kinases (DGKs) are a family of enzymes which phosphorylate diacylglycerol (DAG) to produce phosphatidic acid (PA), thus turning off and on DAG-mediated and PA-mediated signaling pathways, respectively. DGK α activity is stimulated by growth factors and oncogenes and is required for chemotactic, proliferative, and angiogenic signaling in vitro. Herein, using either specific siRNAs or the pharmacological inhibitor R59949, we demonstrate that DGK α activity is required for 17-β-estradiol (E2)-induced proliferation, motility, and anchorage-independent growth of …

medicine.medical_specialtyGPR30medicine.drug_classCell SurvivalDiacylglycerol kinaseMotilityEstrogen receptorEnzyme AssayEndometrial carcinomaBiologyQuinazolinoneReceptors G-Protein-CoupledPiperidinePiperidinesCell MovementInternal medicineCell Line TumormedicineCell AdhesionHumansEndometrial NeoplasmEnzyme AssaysQuinazolinonesDiacylglycerol kinaseCell ProliferationEstradiolCell growthKinaseCell BiologyDiacylglycerol kinase; Endometrial carcinoma; Estrogen; GPR30; Cell BiologyEstrogenEndometrial NeoplasmsCell biologyEnzyme ActivationLipoprotein LipaseEndocrinologyReceptors EstrogenEstrogenGene Knockdown TechniquesGene Knockdown TechniqueFemaleRNA InterferenceSignal transductionGPERHuman
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Acetylcholine mediates the release of IL-8 in human bronchial epithelial cells by a NFkB/ERK-dependent mechanism

2007

Acetylcholine may play a role in cell activation and airway inflammation. We evaluated the levels of both mRNA and protein of muscarinic M(1), M(2), M(3) receptors in human bronchial epithelial cell line (16HBE). 16HBE cells were also stimulated with acetylcholine and extracellular signal-regulated kinase1/2 (ERK1/2) and NFkB pathway activation as well as the IL-8 release was assessed in the presence or absence of the inhibitor of Protein-kinase (PKC) (GF109203X), of the inhibitor of mitogenic activated protein-kinase kinase (MAPKK) (PDO9805), of the inhibitor of kinaseB-alpha phosphorilation (pIkBalpha) (BAY11-7082), and of muscarinic receptor antagonists tiotropium bromide, 4-Diphenylacet…

medicine.medical_specialtyIndolesNeutrophilsScopolamine DerivativesBronchiMuscarinic AntagonistsBiologyPharmacologyMaleimideschemistry.chemical_compoundPiperidinesInternal medicineNitrilesMuscarinic acetylcholine receptor M5Muscarinic acetylcholine receptormedicineHumansRNA MessengerSulfonesTiotropium BromideProtein Kinase CCell Line TransformedAcetylcholine receptorFlavonoidsMitogen-Activated Protein Kinase 1PharmacologyMitogen-Activated Protein Kinase 3Gallamine TriethiodideInterleukin-8NF-kappa BMuscarinic acetylcholine receptor M3Epithelial CellsMuscarinic acetylcholine receptor M2PirenzepineMuscarinic acetylcholine receptor M1Receptors MuscarinicAcetylcholineChemotaxis LeukocyteEndocrinologychemistryTelenzepineAcetylcholinemedicine.drugEuropean Journal of Pharmacology
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Induction of c-fos gene expression by the selective sigma receptor ligand EMD 57445 in rat brain.

1996

Based on animal studies it has been reasoned that ligands to sigma binding sites might be effective in the treatment of schizophrenic disorders and may also be used to investigate this largely elusive disorder on a molecular level. Expression patterns of c-fos in rat brain were studied following treatment with single doses of the sigma ligand EMD 57445 (0.3, 1, 3, 30 mg/kg s.c.). Specific c-fos gene expression was detected at all concentrations tested in various cortical areas. The signals observed were dose-dependent with the highest intensities in the piriform cortex. Strong signals were also detected in hippocampal areas CA 1,2,3 and the gyrus dentatus, as well as in the medial habenula …

medicine.medical_specialtyMammillary bodyNucleus accumbensHippocampal formationc-FosHippocampusRats Sprague-DawleyPiperidinesPiriform cortexInternal medicinemedicineAnimalsReceptors sigmaPharmacology (medical)OxazolesBiological PsychiatryIn Situ HybridizationPharmacologybiologyDose-Response Relationship DrugChemistryOlfactory tubercleBrainRatsPsychiatry and Mental healthEndocrinologyNeurologyHypothalamusIslands of Callejabiology.proteinFemaleNeurology (clinical)Proto-Oncogene Proteins c-fosAntipsychotic AgentsEuropean neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology
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