Search results for "ISM [radio lines]"

showing 10 items of 1018 documents

Interactions of benzodiazepines with human serum albumin. Circular dichroism studies.

1973

The circular dichroism spectra of 12 benzodiazepine derivatives studied in presence of human serum albumin are presented. Nearly all substances give biphasic extrinsic Cotton effects. At the CD maxima the molar ellipticities and the anisotropy factors are calculated. The influence of the chemical structure of the benzodiazepines on the induced Cotton effect is discussed. There is a linear correlation between the anisotropy factors and the logarithms of the partition coefficients of the substances. It is suggested that the phenyl ring of the benzodiazepine molecule is one of the essential groups for the binding of these substances to human serum albumin.

PharmacologyBenzodiazepineCircular dichroismChromatographyBinding SitesChemistrymedicine.drug_classChemical structureCircular DichroismGeneral MedicineBenzazepinesHuman serum albuminCircular dichroism spectraPartition coefficientStructure-Activity RelationshipOptical Rotatory DispersionmedicineMoleculeHumansSpectrophotometry UltravioletChlorineCotton effectSerum Albuminmedicine.drugProtein BindingNaunyn-Schmiedeberg's archives of pharmacology
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�ber den Einflu� von Digitoxigenin auf das Aktionspotential des Vorhofs euthyreoter und hyperthyreoter Meerschweinchen bei experimentellen Insuffizie…

1961

An isolierten Herzohren von Meerschweinchen wurden intracellulare Aktionspotentiale unter gleichzeitiger Registrierung der Kontraktionen abgeleitet. Untersucht wurde der Einflus des Digitoxigenins nach Barbituratschadigung und unter Calciummangel bei euthyreoten und hyperthyreoten Tieren.

PharmacologyCalcium Metabolism DisordersAtrium (architecture)business.industryPharmacology toxicologyGeneral MedicinePharmacologymedicine.diseaseDigitoxigeninchemistry.chemical_compoundchemistryHeart failuremedicineEuthyroidDIGITALIS GLYCOSIDESbusinessHeart atriumNaunyn-Schmiedeberg's Archiv f�r Experimentelle Pathologie und Pharmakologie
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In vivo hypotensive activity ofPistacia lentiscus L

1988

The present studies were undertaken to explain the mechanism of action of the hypothesive effect of Pistacia lentiscus L. aqueous extract. The potassium, calcium and magnesium content of the aqueous extract was determined and synthetic mixtures of salts evaluated in rats. The urinary excretion volume and the sodium and potassium concentrations in urine were also determined. In an effort to explain the effects of the extract, in vivo pharmacological experiments were conducted.

PharmacologyChromatographybiologyTraditional medicineMagnesiumSodiumPotassiumchemistry.chemical_elementUrineCalciumbiology.organism_classificationMechanism of actionchemistryIn vivoPistacia lentiscusmedicinemedicine.symptomPhytotherapy Research
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Vasodilator Effects of Liriodenine and Norushinsunine, Two Aporphine Alkaloids Isolated from <i>Annona cherimolia,</i>in Rat Aorta

1995

The effect of two aporphines, liriodenine and norushinsunine, isolated from Annona cherimolia, were studied in the rat aorta in order to examine their mechanism of action. Both alkaloids (10–7–10–4 mol/l) showed relaxant effects on the contractions elicited by 10–6 mol/l noradrenaline (NA) or 80 mmol/l KC1, but, while liriodenine showed a nonspecific relaxant action on both spasmogens, norushinsunine was more potent on KC1-induced contraction. In Ca2+-free medium, both alkaloids (0.1 mmol/l) inhibited the responses elicited by NA, but not those elicited by caffeine. This inhibitory action occurred when the alkaloids were present during the release of the Ca2+ internal stores or during the r…

PharmacologyContraction (grammar)biologyChemistryLiriodenineGeneral MedicineAporphinesPharmacologyInhibitory postsynaptic potentialbiology.organism_classificationchemistry.chemical_compoundMechanism of actionAnnonaceaemedicineChannel blockermedicine.symptomCaffeinePharmacology
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The nitric oxide related therapeutic phenomenon: a challenging task.

2002

Nitric oxide (NO), produced from L-arginine by the activity of constitutive and inducible NO synthases, has been implicated in a wide range of physiological and pathophysiological processes. Low concentrations of this mediator play homeostatic roles, whereas NO is up-regulated in a number of pathological states and can have damaging effects. Pharmacological modulation of NO levels or NO biosynthesis may be a therapeutic strategy for a number of conditions, although the reported results can be some times controversial. Inhibitors of NO synthases exhibit different selectivity for the neuronal, endothelial or inducible isoforms, which contributes to their beneficial and detrimental effects. Re…

PharmacologyGene isoformbiologyInflammationNitric OxideNitric oxideNitric oxide synthasePathogenesischemistry.chemical_compoundMediatorchemistryMechanism of actionDrug DiscoveryImmunologymedicinebiology.proteinAnimalsHumansmedicine.symptomNeuroscienceHomeostasisCurrent pharmaceutical design
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Role of nuclear factor-κB and heme oxygenase-1 in the mechanism of action of an anti-inflammatory chalcone derivative in RAW 264.7 cells

2004

The synthetic chalcone 3',4',5',3,4,5-hexamethoxy-chalcone (CH) is an anti-inflammatory compound able to reduce nitric oxide (NO) production by inhibition of inducible NO synthase protein synthesis. In this work, we have studied the mechanisms of action of this compound. CH (10-30 microm) prevents the overproduction of NO in RAW 264.7 macrophages stimulated with lipopolysaccharide (1 microg ml(-1)) due to the inhibition of nuclear factor kappaB (NF-kappaB) activation. We have shown that treatment of cells with CH results in diminished degradation of the NF-kappaB-IkappaB complex leading to inhibition of NF-kappaB translocation into the nucleus, DNA binding and transcriptional activity. We a…

PharmacologyOxygenaseChalconebiologyChemistryNFKB1Nitric oxideHeme oxygenaseNitric oxide synthasechemistry.chemical_compoundBiochemistryMechanism of actionmedicinebiology.proteinmedicine.symptomHemeBritish Journal of Pharmacology
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Flupirtine increases the levels of glutathione and Bcl-2 in hNT (human ) neurons: mode of action of the drug-mediated anti-apoptotic effect

1996

Flupirtine is a triaminopyridine analogue which has been successfully applied in clinics as a non-opiate analgesic drug. Previously we described that flupirtine acts like an N-methyl-D-aspartate (NMDA) receptor antagonist in neuronal cells both in vitro and in vivo. Here we show that flupirtine displays its anti-apoptotic effect also in hNT (human Ntera/D1) neurons. hNT neurons were induced to apoptosis applying glutamate (Glu; at concentrations > or = 1 mM) or NMDA (> or = 1 mM). During Glu/NMDA-mediated apoptosis the levels of the intracellular anti-apoptotic agents Bc1-2 and glutathione dropped by more than 50%. Flupirtine completely abolished this reduction of Bc1-2 and glutathione leve…

PharmacologyProgrammed cell deathChemistrymedicine.drug_classGlutamate receptorGlutathionePharmacologyReceptor antagonistchemistry.chemical_compoundmedicine.anatomical_structurenervous systemBiochemistryMechanism of actionmedicineNMDA receptorNeuronFlupirtinemedicine.symptommedicine.drugEuropean Journal of Pharmacology
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Ah receptor mediating induction of cytochrome P450IA1 in a novel continuous human liver cell line (Mz-Hep-1)

1991

Abstract The Ah receptor regulates induction of cytochrome P450IA1 and mediates certain toxicities of polyhalogenated aromatics such as 2,3,7,8-tetrachlorodibenzo- p -dioxin (TCDD). It has been characterized previously in continuous cell lines, notably the mouse hepatoma line Hepa 1, the human squamous cell carcinoma line A431, and the human liver cell line Hep G2. The present work extends our knowledge of the Ah receptor in continuous human liver cell lines. Ah receptor can be detected in Mz-Hep-1, a hepatitis B virus-negative cell line derived from a Thorotrast-induced hepatocellular carcinoma. The mean concentration of Ah receptor in Mz-Hep-1 cells was 341 ± 22 fmol/mg cytosol protein (m…

PharmacologyReceptor complexChemistryEstrogen receptorBiochemistryHep G2Dissociation constantGlucocorticoid receptorMechanism of actionBiochemistryCell culturemedicinemedicine.symptomGlucocorticoidmedicine.drugBiochemical Pharmacology
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Aminobisphosphonates as New Weapons for γ δ T Cell-Based Immunotherapy of Cancer

2008

Several observations in mice and in humans have collectively laid the foundation for examining the potential of γ δ T cells to exert tumor immunotherapy. Human γ δ T cells can be activated in a non-MHC dependent fashion either by low molecular mass phosphoantigens, or by agents that provoke the accumulation of endogenous pyrophosphates such as isopentenylpyrophosphate. Among the latter, aminobisphosphonates are well-established in the clinic, and extensive data are available on the compounds antiangiogenic, antiosteolytic and pro-apoptotic properties. In this review we discuss on the possibility that the intentional activation of γ δ T cells in vivo by aminobisphosphonates may represent a p…

Pharmacologybusiness.industrymedicine.medical_treatmentT cellOrganic ChemistryCancerEndogenyImmunotherapyT lymphocytemedicine.diseaseBiochemistrymedicine.anatomical_structureMechanism of actionAntigenIn vivoDrug DiscoveryImmunologymedicineMolecular Medicinemedicine.symptombusinessCurrent Medicinal Chemistry
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Selective Modulation of Aβ42 Production in Alzheimers Disease: Non-Steroidal Anti-Inflammatory Drugs and Beyond

2006

The amyloid-β (Aβ) peptides and in particular the longer, highly amyloidogenic isoform Aβ42 are believed by many to be the central disease-causing agents in Alzheimers disease (AD). Consequently, academic and pharmaceutical laboratories have focused on elucidating the mechanisms of Aβ production and developing strategies to diminish Aβ formation for treatment or prevention of AD. The most substantial advances have been made with respect to inhibitors of the γ-secretase enzyme, which catalyzes the final step in the generation of Aβ from the amyloid precursor protein (APP). Highly potent γ-secretase inhibitors which suppress production of all Aβ peptides are available today. However, due to t…

Pharmacologychemistry.chemical_classificationGene isoformbiologybusiness.industryNotch signaling pathwayPharmacologymedicine.diseaseSmall moleculePathogenesisEnzymechemistryMechanism of actionDrug DiscoveryImmunologymedicineAmyloid precursor proteinbiology.proteinAlzheimer's diseasemedicine.symptombusinessCurrent Pharmaceutical Design
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