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  • Chemistry  (37)
  • ATP-sensitive potassium channel  (2)
  • Cyclic AMP formation  (2)
  • 1
    ISSN: 1432-1912
    Keywords: Dispersion ; Refractoriness ; ATP-sensitive potassium channel ; Canine ; Programmed electrical stimulation
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The proarrhythmic effects of the ATP-sensitive potassium channel modulators cromakalim (n = 10; 0.01 to 0.3 mg/kg i.v.), glibenclamide (n = 10; 0.3 to 10 mg/kg i.v.) or volume equivalents of vehicle (n = 10) were evaluated in post-infarcted anaesthetised dogs. Dogs were anaesthetised, subjected to an anterior-apical myocardial infarction, and allowed to recover. At 7.4 ± 0.7 days post infarction, animals were anaesthetised again, electrophysiologic measurements (effective refractory periods, QT-intervals and ventricular fibrillation thresholds) were taken, and animals were tested for arrhythmias using a programmed electrical stimulation protocol. Only animals that did not have programmed electrical stimulation-inducible arrhythmias were used. Ventricular fibrillation thresholds were determined twice, once before the first dose then after the last dose of drug. At the end of the experiment, animals were subjected to ligation of the left circumflex coronary artery and survival was measured over the next two hours. Cromakalim significantly increased heart rate and decreased blood pressure. Although cromakalim significantly reduced effective refractory periods, it neither increased electrical dispersion, as determined by the standard deviation or coefficient of variance of the effective refractory period, nor did it enhance inducibility (0 out of 10 in both vehicle and cromakalim treated animals), change ventricular fibrillation thresholds, or reduce sudden death survival relative to vehicle. Glibenclamide did not increase electrical dispersion, but slightly increased the incidence of programmed electrical stimulation-induced arrhythmias (3 out of 10), and lowered ventricular fibrillation thresholds values. However, these changes were not statistically significant. Glibenclamide did not significantly affect survival relative to vehicle. Infarct sizes of the left ventricle were not statistically different among groups. In conclusion, cromakalim and glibenclamide did not affect dispersion of refractoriness. Glibenclamide did demonstrate a propensity towards proarrhythmic activity. However, the doses needed to observe proarrhythmic activity with glibenclamide were significantly higher than those needed for clinical treatment of hyperglycemia.
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  • 2
    ISSN: 1432-1912
    Keywords: Key words Dispersion ; Refractoriness ; ATP-sensitive potassium channel ; Canine ; Programmed electrical stimulation
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract  The proarrhythmic effects of the ATP-sensitive potassium channel modulators cromakalim (n=10; 0.01 to 0.3 mg/kg i.v.), glibenclamide (n=10; 0.3 to 10 mg/kg i.v.) or volume equivalents of vehicle (n=10) were evaluated in post-infarcted anaesthetised dogs. Dogs were anaesthetised, subjected to an anterior-apical myocardial infarction, and allowed to recover. At 7.4±0.7 days post infarction, animals were anaesthetised again, electrophysiologic measurements (effective refractory periods, QT-intervals and ventricular fibrillation thresholds) were taken, and animals were tested for arrhythmias using a programmed electrical stimulation protocol. Only animals that did not have programmed electrical stimulation-inducible arrhythmias were used. Ventricular fibrillation thresholds were determined twice, once before the first dose then after the last dose of drug. At the end of the experiment, animals were subjected to ligation of the left circumflex coronary artery and survival was measured over the next two hours. Cromakalim significantly increased heart rate and decreased blood pressure. Although cromakalim significantly reduced effective refractory periods, it neither increased electrical dispersion, as determined by the standard deviation or coefficient of variance of the effective refractory period, nor did it enhance inducibility (0 out of 10 in both vehicle and cromakalim treated animals), change ventricular fibrillation thresholds, or reduce sudden death survival relative to vehicle. Glibenclamide did not increase electrical dispersion, but slightly increased the incidence of programmed electrical stimulation-induced arrhythmias (3 out of 10), and lowered ventricular fibrillation thresholds values. However, these changes were not statistically significant. Glibenclamide did not significantly affect survival relative to vehicle. Infarct sizes of the left ventricle were not statistically different among groups. In conclusion, cromakalim and glibenclamide did not affect dispersion of refractoriness. Glibenclamide did demonstrate a propensity towards proarrhythmic activity. However, the doses needed to observe proarrhythmic activity with glibenclamide were significantly higher than those needed for clinical treatment of hyperglycemia.
    Type of Medium: Electronic Resource
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  • 3
    ISSN: 1432-1912
    Keywords: Amphetamine ; Dopamine release ; Corpus striatum ; Dopamine receptors ; Cyclic AMP formation
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Changes in the formation of cyclic AMP following d-amphetamine (0.1 to 20 pmol/1) were examined in vitro in striatal slices of the rat. d-Amphetamine caused a doserelated increase in cyclic AMP content. This action of d-amphetamine was abolished by tissue pretreatment with reserpine (2.5 mg/kg, i.p.) and 3-iodotyrosine (1 mmol/1). By contrast, both clorgyline (0.1 pmol/l) and nomifensine (30 μmol/l) enhanced the d-amphetamine-induced increase in cyclic AMP formation. In superfusion experiments, a strong correlation between endogenous dopamine and cyclic AMP release was observed before, during and after d-amphetamine exposure. Finally, Sch 23390 (10 μmol/1) abolished while (−)sulpiride (10 μmol/1) enhanced the amphetamine-induced increase in cyclic AMP content. These results suggest that d-amphetamine enhances the formation of cyclic AMP through the release of endogenous dopamine into the synapse where it can interact with both D-1 and D-2 dopamine receptors. These results provide direct evidence that the antagonistic properties of D-1 and D-2 receptors on cyclic AMP formation are apparent at striatal synapses during release of endogenous neuronal dopamine.
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  • 4
    ISSN: 1432-1912
    Keywords: Amphetamine ; Dopamine receptors ; Cyclic AMP formation ; Monoamine oxidase ; Corpus striatum
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The roles of multiple forms of monoamine oxidase (MAO) in regulating the synaptic concentration of dopamine, in the vicinity of dopamine receptors associated with cyclic AMP formation, was examined in striatal slices of the rat. d-Amphetamine (0.1 μmol/l to 20 μmol/l) caused a concentration-related increase in cyclic AMP formation, which correlated (in superfusion experiments) with the release of endogenously-formed dopamine. In the presence of (−)sulpiride (50 pmol/l), cyclic AMP formation was significantly increased at every concentration of d-amphetamine tested. At the same time, this concentration of (−)sulpiride had no effect on DA release. Inhibition of type A MAO with clorgyline (0.1 μmol/l) significantly enhanced the increase in cyclic AMP formation seen after d-amphetamine. By contrast, inhibition of type B MAO with deprenyl (0.1 μmol/l) was without effect on this action of d-amphetamine. At high concentrations of d-amphetamine (20 μmol/l), however, deprenyl + clorgyline treatment enhanced cyclic AMP formation to a greater extent than with clorgyline alone. Similar results could be obtained at lower concentrations of d-amphetamine (5 μmol/l), but only after inhibition of the dopamine neuronal reuptake system with nomifensine (30 gmol/1). Furthermore, in the presence of nomifensine, deprenyl alone was also able to significantly increase the cyclic AMP formation seen after d-amphetamine (5 gmol/l). In the presence of (−)sulpiride, relatively similar results were obtained following all MAO inhibitor treatments. These findings support the notion that type A MAO plays the primary role in regulating dopamine concentrations at D-1 and D-2 receptors within synapses of rat striatal tissue. However, a minor role for type B MAO can be demonstrated when high synaptic concentrations of dopamine are achieved or dopamine deamination is restricted to postsynaptic sites. Experiments with amezinium (10 μmol/l) were conducted to further explore the importance of presynaptic and postsynaptic type A MAO in the regulation of synaptic concentrations of dopamine; total type A MAO inhibition was assessed with clorgyline (0.1 μmol/l). caused a two-fold increase in the ability of d-amphetamine (5 μmol/l) to increase cyclic AMP formation. This result represented 70% of the response obtained after total type A MAO inhibition with clorgyline. The values obtained with clorgyline, but not amezinium, were potentiated by inhibition of the dopamine neuronal reuptake system with nomifensine. These results support the idea that presynaptic type A MAO is highly instrumental in regulating synaptic dopamine concentrations; possibly by regulating the size of the pool of releasable dopamine. Postsynaptic type A MAO, however, can also play an effective role in the regulation of synaptic DA levels in instances where the dopamine neuronal reuptake system may become compromised.
    Type of Medium: Electronic Resource
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  • 5
    Electronic Resource
    Electronic Resource
    New York : Wiley-Blackwell
    Die Makromolekulare Chemie 182 (1981), S. 3351-3359 
    ISSN: 0025-116X
    Keywords: Chemistry ; Polymer and Materials Science
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology , Physics
    Notes: A distinct improvement of the tensile properties of “surface growth” polyethylene fibers can be realised by drawing at elevated temperatures. The optimal drawing temperatures were found in the range of 120-150°C. Drawing in the hexagonal phase above 150°C does not lead to an increase of strength. Elongational viscosity measurements revealed extremely high values in the order of 1011-1012 Poise. Activation energies between 75-95 kJ/mol were determined from the temperature dependence of elongational viscosity. The observed drawing behaviour is discussed in relation to the morphological changes that occur during drawing.
    Additional Material: 5 Ill.
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  • 6
    ISSN: 0025-116X
    Keywords: Chemistry ; Polymer and Materials Science
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology , Physics
    Notes: The bulk polymerization of L,L-dilactide was studied as a function of polymerization temperature (Tp), time and concentration of catalyst (tin 2-ethylhexanoate). Poly(L-lactide) (PLLA), with the highest value of intrinsic viscosity ([η] = 13 dl · g-1; M̄v ≈ 1 · 106) and heat of fusion (ΔHm = 64,7 J · g-1), was synthesized at a low catalyst concentration (0,015 wt.-%) and at the lowest Tp studied (100°C), just above the melting point of L,L-dilactide (98°C). The ceiling temperature of PLLA was found to be 275°C, as deduced from an M̄v max. - Tp curve. The M̄w/M̄n ratios of as-polymerized PLLA samples ranged from 2 to 3. Fractions of PLLA with M̄v max. were already present at 50% conversion. The experimental results support a proposed nonionic insertion polymerization mechanism. Polymerization at 100-140°C resulted in early crystallization of PLLA leading to a rather untangled polymer and microporous (pores up to 100 nm) sample texture.
    Additional Material: 4 Ill.
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  • 7
    Electronic Resource
    Electronic Resource
    New York, NY [u.a.] : Wiley-Blackwell
    Journal of Applied Polymer Science 9 (1965), S. 1579-1584 
    ISSN: 0021-8995
    Keywords: Chemistry ; Polymer and Materials Science
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology , Mechanical Engineering, Materials Science, Production Engineering, Mining and Metallurgy, Traffic Engineering, Precision Mechanics , Physics
    Notes: In a previous paper it was shown that the vulcanization obtained with ethylene-propylene-diene terpolymer is equivalent or superior to that obtained with ethylene-propylene copolymer when a peroxide-dimethacrylate coagent cure system was used. In order to determine the effect of the unsaturation on the physical properties in the terpolymer, the terpolymer had been hydrogenated to remove the double bonds. Infrared spectra and bromination were used to check the extent of hydrogenation. Tensile strength, Shore A hardness, per cent elongation, and modulus indicated no decrease in vulcanization efficiency after hydrogenation. The data show that the unsaturation in the terpolymer does not contribute to the vulcanization cure with the peroxide-dimethacrylate coagent curing system.
    Additional Material: 1 Ill.
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  • 8
    Electronic Resource
    Electronic Resource
    New York, NY : Wiley-Blackwell
    Proteins: Structure, Function, and Genetics 2 (1987), S. 130-152 
    ISSN: 0887-3585
    Keywords: amino acid hydophobicity scale ; QSAR ; amino acids ; peptide side chains ; Chemistry ; Biochemistry and Biotechnology
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Medicine
    Notes: The fragment method of calculation partition coefficients (P) has been extended to include the common amino acids (AAs). The results indicate that polar and charged side chains influence the hydrophobicity of atoms in the side chain in a predictable manner. Feild effects, as evidenced through polar proximity factors and bond factors, need to be considered for accurate estimation of transfer phenomena. The calculated log P and ΔG°′ values of the 20 AAs agree well with the observed values. Pro calculates to be more hydrophilic than the observed log P. Hydrophobicity scales for peptide side chain residues are compared and evaluated in terms of suitability. Calculated π values for nonpolar side chain residures agree well with the observed values; calculated values for uncharged polar side chain residues deviate by about 0.6 log units except for Gln and Cys; and polar side chain residues with charged side chains calculate as too hydorphilic. Reasons for the differences are explored. We also suggest that tightly bound water to polar moieties in amino acids and peptides may be transferred into the octanol phase during partitioning experiments. A quantitative methodology is persented which characterizes the thermodynamic partitioning of groups and individual atoms in amino acids and proteins.
    Additional Material: 7 Ill.
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  • 9
    Electronic Resource
    Electronic Resource
    Bognor Regis [u.a.] : Wiley-Blackwell
    Journal of Polymer Science Part A: Polymer Chemistry 33 (1995), S. 493-504 
    ISSN: 0887-624X
    Keywords: butanediol ; 4,4′-biphenyldicarboxylic acid ; characterization ; liquid crystalline polymer ; methyl substitution ; nematic ; polyester ; smectic ; synthesis ; thermal properties ; X-ray analysis ; Chemistry ; Polymer and Materials Science
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: Results are reported on the effect of lateral methyl groups on the thermal properties of a series of polyesters prepared from diethyl 4,4′-biphenyldicarboxylate and various methyl substituted 1,4-butanediols. The diols were 1,4-butanediol; 2-methyl-1,4-butanediol; 2,2-dimethyl-1,4-butanediol; 2,3-dimethyl-1,4-butanediol; 2,2,3-trimethyl-1,4-butanediol; and 2,2,3,3-tetramethyl-1,4-butanediol. Apart from the tetramethyl derivatve, the transition temperatures of the methyl substituted polyesters were lower with respect of the unsubstituted polyester. On the basis of polarized photomicrographs, a smectic A mesophase was found for the unsubstituted polyester, whereas a nematic mesophase was observed for the 2-methyl substituted polyster. The 2,2-dimethyl, 2,3-dimethyl, and the 2,2,3-trimethyl substituted polyesters showed no liquid crystalline behavior. The 2,2,3,3-tetramethyl derivative displayed a birefringent melt phase although the DSC measurements were not unambiguous. A copolyester based on diethyl 4,4′-biphenyldicarboxylate, 1,4-butanediol, and 2,2,3,3-tetramethyl-1,4-butanediol showed a broad nematic mesophase. Further evidence for the nematic mesophase of this copolyester and the 2-methyl substituted polyester was provided by dynamic rheological experiments. Based on thermogravimetric analysis, it was concluded that the thermal stability was affected only when four methyl side groups were present in the spacer. © 1995 John Wiley & Sons, Inc.
    Additional Material: 8 Ill.
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  • 10
    Electronic Resource
    Electronic Resource
    New York, NY [u.a.] : Wiley-Blackwell
    Biotechnology and Bioengineering 38 (1991), S. 813-820 
    ISSN: 0006-3592
    Keywords: loading rate ; growth yield ; oxidation rate ; free-cell suspensions ; Chemistry ; Biochemistry and Biotechnology
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Biology , Process Engineering, Biotechnology, Nutrition Technology
    Notes: Kinetic parameters of biological sulfide oxidation are described. The influence of the sulfide loading rate on growth yield and specific oxidation rate were investigated with free-cell suspensions. It is concluded that at least two types of bacteria were present, namely, sulfate producers (type A) that grow at higher loading rates. Type A bacteria have a growth yield of 04 g dry S/mol S, while type B bacteria have a growth yield of 04 g dry S/mol S. Type A has a high affinity for sulfide and is inhibited by sulfide at sulfide concentrations exceeding 10 mg/L. Type B has a low affinity for sulfide and is not inhibited by sulfide, but by oxygen.
    Additional Material: 5 Ill.
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