Search results for "AGLA"

showing 10 items of 272 documents

Novel Insights and Therapeutical Applications in the Field of Inhibitors of COX-2

2004

The discovery of the two isoenzymes COX-1 and COX-2 and the knowledge of their function, localisation and regulation has initiated the development of COX-2 selective inhibitors (coxibs). Inducible COX-2 at the peripheral site of inflammation has been detected in the early 1990s, the involvement of recently detected spinal COX-2 has led to new insights into mechanisms of pain and may explain analgesic and antipyretic properties of COX-2 selective inhibitors. The coxibs rofecoxib and celecoxib have been introduced into therapy and seem to offer some advantages over the classical non-selective NSAIDs. The search for new COX-2 inhibitors is going on, the development of etoricoxib and lumiracox…

AnalgesicArthritisPharmacologyBioinformaticsBiochemistryProstate cancerDrug DiscoverymedicineAnimalsHumansCyclooxygenase InhibitorsRofecoxibPharmacologyCyclooxygenase 2 Inhibitorsbusiness.industryOrganic ChemistryMembrane Proteinsmedicine.diseaseTolerabilityCyclooxygenase 2Prostaglandin-Endoperoxide SynthasesCelecoxibMolecular MedicineLumiracoxibbusinessEtoricoxibmedicine.drugCurrent Medicinal Chemistry
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Synthesis of complement by macrophages and modulation of their functions through complement activation.

1983

During the last decade considerable progress has been made to characterize intimate functional links between macrophages, a major cellular component of immunoinflammatory responses, and the complement system representing the major humoral mediator of inflammation. Macrophages of various species and tissue sites have been shown to synthesize and release most of the complement components providing these cells with their own \ldpericellular\rd complement system. Circumstantial evidence for the assembly of both classical and alternative pathway convertases has been adduced. An intricate network of feedback loops involving endogenous and extrinsic factors operates to adjust complement production…

AnaphylatoxinsImmunologyComplement Pathway AlternativeGuinea PigsComplement receptorBiologyIn Vitro TechniquesMonocytesClassical complement pathwayMiceImmune systemPhagocytosisComplement C1AnimalsHumansAnaphylatoxinComplement ActivationComplement component 3MacrophagesComplement C5Complement C4General MedicineComplement C3Complement System ProteinsComplement C2Complement systemCell biologyReceptors ComplementImmunologyAlternative complement pathwayComplement C3aProstaglandinsComplement component 5aSpringer seminars in immunopathology
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Effects of cimetidine, atropine and prostaglandin E2 on rat mucosal erosions produced by intragastric distension

1980

Abstract The effects of three typical antisecretory agents: cimetidine, atrophine and prostaglandin E2 were compared on an acute rat gastric ulcer model which consisted of perfusing the stomach continuously, at a high intraluminal pressure (120 mm H2O), with a simulated gastric juice (0.1 M HCl plus 600 mg pepsin/1). As the acid and pepsin are given exogenously the inhibitory action of the antisecretory drugs is obviated in this model. Cimetidine and atropine failed to reduce gastric erosions, whereas prostaglandin E2 markedly reduced the severity of the mucosal lesions with respect to control values. Long-term treatment with cimetidine also failed to increase the resistance of the gastric …

AtropineMalemedicine.medical_treatmentPharmacologyGuanidinesPepsinmedicineGastric mucosaAnimalsStomach UlcerProstaglandin E2CimetidinePharmacologyGastric Juicebiologybusiness.industryProstaglandins EGastric distensionStomachdigestive oral and skin physiologyRatsDisease Models AnimalAtropinemedicine.anatomical_structureAnesthesiabiology.proteinmedicine.symptomCimetidinebusinessProstaglandin Emedicine.drugEuropean Journal of Pharmacology
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Apmaksāta un neapmaksāta atvaļinājuma tiesiskais regulējums un tā piemērošanas aktualitātes.

2021

Darba autore: Santa Orbidāne Darba tēma: Apmaksāta un neapmaksāta atvaļinājuma tiesiskais regulējums un tā piemērošanas aktualitātes Darba veids: Bakalura darbs Darbs izklāstīts uz 40 lappusēm, ietver 8 tabulas, 20 literatūras avoti. Bakalaura darbā tiek pētīts apmaksāta un neapmaksāta atvaļinājuma tiesiskais regulējums un tā piemērošana. Pētījuma ietvaros, tika aplūkoti atvaļinājuma veidi, to piešķiršana, atlīdzināšana, kā arī darba strīdi. Darba strīdi vienmēr ir aktuāli, bet valstī esošās ārkārtējās situācijas dēļ ir ietekmēti dažādu darba nozaru sfērā strādājošie. Līdz ar to darba mērķis ir izprast, kā rīkoties pareizāk, nepārkāpjot darba ņēmēja tiesības un ko darīt gadījumā, ja šīs tie…

Atvaļinājums bez darba algas saglabāšanasAtpūtas laiksDarba laiksIkgadējais apmaksātais atvaļinājumsJuridiskā zinātnePapildatvaļinājums
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Informācija un sabiedrība: Informācijas un bibliotēku studiju nodaļas raksti : Nr.2

2011

Turpinājumizdevuma „Informācija un sabiedrība: Informācijas un bibliotēku studiju nodaļas raksti” otrajam numuram ir divas daļas. Pirmajā daļā „Nacionālā identitāte digitālā vidē” ir iekļauti raksti, kuros analizēti valsts pētījumu programmas „Nacionālā identitāte (valoda, Latvijas vēsture, kultūra un cilvēkdrošība)” projektā „Nacionālā identitāte un komunikācija” apakšprojektā „Nacionālā identitāte digitālā vidē” veikto pētījumu rezultāti. Otrajā daļā „Bibliotēku darba aspekti” ir raksti, kuru autori ir Latvijas Universitātes bibliotēkas darbinieki. Rakstos analizēti pētījumu rezultāti vairākās ar bibliotēkas darbu saistītās jomās: 1) bibliotēkas pakalpojumi, to transformācija ‘Tīmekļa 2.0…

Bibliotēkas--Sabiedriskās attiecībasInformācijas zinātneDigitālās kolekcijasNacionālā identitāteBibliotēku materiāli--DigitalizācijaBibliotēku personāla vadībaDigitālās bibliotēkasBibliotēkzinātneBibliotēku darbiniekiKolektīvā atmiņaDigitālā saglabāšanaNacionālisms
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Heme oxygenase-1 induction by nitric oxide in RAW 264.7 macrophages is upregulated by a cyclo-oxygenase-2 inhibitor.

2001

Unstimulated RAW 264.7 macrophages express negligible heme oxygenase-1 (HO-1) protein but incubation with the nitric oxide (NO) donor spermine nonoate (SPNO) induced HO-1 and weakly cyclo-oxygenase-2 (COX-2) protein. This effect was potentiated by coincubation with the COX-2 selective inhibitor, SC58125. Cells incubated with SPNO showed a strong increase in HO-1 mRNA levels after 4 h with a significant potentiation in the presence of SC58125, which did not modify HO-1 mRNA stability. The induction of HO-1 by NO and its potentiation by anti-inflammatory agents may play a role in inflammatory and immune responses.

BiophysicsSpermineNitric OxideBiochemistryNitric oxideCell Linechemistry.chemical_compoundMiceDownregulation and upregulationMacrophageAnimalsCyclooxygenase InhibitorsRNA MessengerMolecular BiologyHemeCyclooxygenase 2 InhibitorsMacrophagesMembrane ProteinsLong-term potentiationDrug SynergismMolecular biologyUp-RegulationHeme oxygenaseIsoenzymeschemistryBiochemistryCell cultureCyclooxygenase 2Prostaglandin-Endoperoxide SynthasesHeme Oxygenase (Decyclizing)PyrazolesNitrogen OxidesSpermineHeme Oxygenase-1Biochimica et biophysica acta
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Mechanisms involved in the relaxant action of testosterone in the renal artery from male normoglycemic and diabetic rabbits.

2009

Kidney disease is a frequent complication in diabetes, and significant differences have been reported between male and female patients. Our working hypothesis was that diabetes might modify the vascular actions of testosterone in isolated rabbit renal arteries and the mechanisms involved in these actions. Testosterone (10(-8) to 10(-4)M) induced relaxation of precontracted arteries, without significant differences between control and diabetic rabbits. Both in control and diabetic rabbits endothelium removal inhibited testosterone relaxant action. In arteries with endothelium, incubation with indomethacin (10(-5)M), N(G)-nitro-l-arginine (10(-5)M) or tetraethylammonium (10(-5)M) did not modi…

Blood GlucoseMalemedicine.medical_specialtyEndotheliumNitric Oxide Synthase Type IIIThromboxaneBlotting WesternIndomethacinNitric Oxide Synthase Type IIProstacyclinVasodilationNitroarginineMuscle Smooth VascularDiabetes Mellitus ExperimentalImmunoenzyme TechniquesThromboxane A2Renal ArteryEnosInternal medicinemedicine.arteryDiabetes mellitusmedicinePotassium Channel BlockersAnimalsCyclooxygenase InhibitorsProstaglandins ITestosteroneRenal arteryPharmacologybiologyDose-Response Relationship Drugbusiness.industryTetraethylammoniumTestosterone (patch)medicine.diseasebiology.organism_classificationVasodilationEndocrinologymedicine.anatomical_structureCyclooxygenase 2Cyclooxygenase 1PotassiumCalciumEndothelium VascularRabbitsbusinessmedicine.drugSignal TransductionPharmacological research
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Synthesis and Evaluation of a Novel Series of Pyrrolizine Derivatives as Dual Cyclooxygenase-1 and 5-Lipoxygenase Inhibitors

1997

The aim of our study was to investigate structure activity relationship following the replacement of the 6-phenyl substituent at the 6,7-diaryl-2,3-dihydropyrrolizine template by various heteroaromatic residues. In this context we developed a new, efficient, and highly sensitive test method for the screening of dual cyclooxygenase-1 (COX-1) and 5-lipoxygenase (5-LOX) inhibitors. We used human platelets as a source of COX-1 and human PMNLs as a source of 5-LOX. Both cell types were isolated from the same volume of blood. PGE2 and LTB4 respectively were determined by highly selective and sensitive ELISA kits, using monoclonal antibodies. For a single determination at most 0.5 mL whole blood i…

Blood PlateletsMaleNeutrophilsmedicine.drug_classPharmaceutical ScienceContext (language use)Monoclonal antibodyChemical synthesisDrug DiscoverymedicineHumansStructure–activity relationshipCyclooxygenase InhibitorsPyrrolesLipoxygenase InhibitorsWhole bloodArachidonate 5-LipoxygenasebiologyChemistryMembrane ProteinsIn vitroIsoenzymesBiochemistryProstaglandin-Endoperoxide SynthasesEnzyme inhibitorArachidonate 5-lipoxygenaseCyclooxygenase 1biology.proteinFemaleArchiv der Pharmazie
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Anti-inflammatory and analgesic activity of a novel inhibitor of microsomal prostaglandin E synthase-1 expression

2009

Abstract In a previous study, we reported a new γ-hydroxybutenolide derivative, 4-benzo[ b ]thiophen-2-yl-3-bromo-5-hydroxy-5 H -furan-2-one (BTH), as inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1) expression in lypopolysaccharide (LPS) stimulated RAW 264.7 and TPH-1 cells, without affecting cyclooxygenase-2 (COX-2). In this study, we evaluated the in vivo effect of BTH on some acute and chronic inflammatory animal models in relation to its inhibitory profile on mPGES-1 expression. In the zymosan-induced mouse air pouch model, BTH produced a dose-dependent inhibition of prostaglandin E 2 (PGE 2 ) production and mPGES-1 protein expression in pouch exudates without any effect on…

Blood PlateletsMaleNeutrophilsmedicine.drug_classmedicine.medical_treatmentAnti-Inflammatory AgentsProstaglandinInflammationThiophenesAcetatesPharmacologyProstaglandin E synthaseLeukotriene B4Gene Expression Regulation EnzymologicAnti-inflammatoryMicechemistry.chemical_compound4-ButyrolactoneIn vivomedicineAnimalsHumansProstaglandin-E SynthasesInflammationPharmacologyAnalgesicsBehavior AnimalbiologyArthritis ExperimentalIntramolecular OxidoreductasesThromboxane B2BiochemistrychemistryHyperalgesiaChronic DiseaseHyperalgesiabiology.proteinCattlelipids (amino acids peptides and proteins)Arachidonic acidmedicine.symptomProstaglandin E
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Cyclooxygenase-1/2 (COX-1/COX-2) and 5-lipoxygenase (5-LOX) inhibitors of the 6,7-diaryl-2,3-1H-dihydropyrrolizine type

2003

A series of 6,7-diaryl-2,3-1H-dihydropyrrolizines was prepared as COX-1/COX-2 and 5-LOX inhibitors. The inhibition of COX-1 was evaluated using intact bovine platelets as the enzyme source, whereas LPS-stimulated human monocytes served as the enzyme source for inducible COX-2. The determination of arachidonic metabolites was performed by HPLC for COX-1 and RIA for COX-2. The balance between COX-1/COX-2 and 5-LOX inhibition can be shifted by modifying the substitution pattern of the phenyl moiety at the 6- and 7-position of the pyrrolizine nucleus. Structure-activity relationships are discussed.

Blood PlateletsRadioimmunoassayHigh-performance liquid chromatographyIsozymeMonocytesDrug DiscoverymedicineCox 1 cox 2AnimalsHumansMoietyStructure–activity relationshipPyrrolesPlateletLipoxygenase InhibitorsEnzyme InhibitorsChromatography High Pressure LiquidPharmacologychemistry.chemical_classificationbiologyChemistryOrganic ChemistryMembrane ProteinsGeneral MedicineIn vitroIsoenzymesmedicine.anatomical_structureEnzymeBiochemistryCyclooxygenase 2Prostaglandin-Endoperoxide SynthasesEnzyme inhibitorDrug DesignArachidonate 5-lipoxygenaseCyclooxygenase 1biology.proteinCattleCyclooxygenaseNucleusEuropean Journal of Medicinal Chemistry
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