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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    Cellular and molecular life sciences 31 (1975), S. 689-691 
    ISSN: 1420-9071
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Zusammenfassung In der löslichen überstehenden Fraktion (105,000×g) der Kopfniere des KnochenfischesAnabas testudineus wurde ein Enzym nachgewiesen, welches die Synthese des Thyroxins katalysiert. Die Menge des löslichen Nierenproteins und die Inkubationszeit stellen zwei limitierende Faktoren für die in vitro-Synthese des Thyroxins dar.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1432-1440
    Keywords: Congestive heart failure ; Left ventricular ejection fraction ; Vasodilating β-blocker
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Several studies in the past have shown the long-term beneficial effects of β-blockers in congestive heart failure. Despite the interest in this mode of therapy, their clinical application has been limited due to their negative inotropic effect. A subset of the heart failure patients do not show any improvements with standard β-blocker therapy. Carvedilol, a new, non-selective β-blocking agent with concurrent α-blocking properties, was evaluated in 17 patients with chronic heart failure secondary to ischaemic heart disease. All had resting left ventricular ejection fraction ≤45% and were maintained on diuretic therapy. Acute haemodynamic measurements were made after intravenous carvedilol (2.5–7.5 mg) and also after chronic therapy for 8 weeks (carvedilol 12.5–50 mg b.d.). Radionuclide ventriculography, ambulatory intra-arterial blood pressure monitoring and right heart catheterization were performed before and after 8 weeks of chronic therapy. Twelve patients completed the study and 5 were withdrawn. Symptomatic and haemodynamic improvement was demonstrated in 11 of the 12 patients after 8 weeks of therapy. Mean±standard error systolic intraarterial blood pressure (133 ± 6 to 114 ± 5 mmHg, P 〈0.005), heart rate (81 ± 3 to 61 ± 1 beats/min, P 〈0.0001), pulmonary artery wedge pressure (19 ± 2 to 12 ± 1 mmHg, P 〈0.001) and systemic vascular resistance (1748 ± 115 to 1497 ± 89 dynes/ s/cm5/m2, P 〈 0.02) were reduced with an increase in mean ± SE of stroke volume index (31 ± 1.8 to 40 ± 1.6 ml/m2/beat, P 〈 0.0005) and left ventricular ejection fraction (25 ± 3 % to 32 ± 3 %, P 〈 0.01) after 8 weeks of therapy with carvedilol. This is in contrast to the acute haemodynamic effects of carvedilol, which only showed a reduction in heart rate (81 ± 3 to 74 ± 3 beats/min, P 〈 0.0001), systolic intra-arterial blood pressure (133 ± 6 to 117 ±6 mmHg, P 〈 0.0005) and pulmonary artery wedge pressure (19 ± 2 to 14 ± 2 mmHg, P 〈 0.002) at 10 min post-injection. The systemic vascular resistance, left ventricular ejection fraction and stroke volume index failed to show any significant improvement. Thus intravenous carvedilol produces a reduction in filling pressure, which is maintained after chronic treatment. This property is clearly beneficial for chronic heart failure patients and differs from standard β-blockers. The discrepancy of the haemodynamic changes between the acute and chronic long-term response to carvedilol lends further support to the concept of upregulation of β-adrenoceptors in cognestive heart failure.
    Type of Medium: Electronic Resource
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  • 3
    Electronic Resource
    Electronic Resource
    Springer
    Microchimica acta 90 (1986), S. 175-186 
    ISSN: 1436-5073
    Keywords: phenol ; total alkali ; FIA ; industrial phenol liquor
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Flow injection analysis (FIA) has been applied to the determination of total phenol and total alkali in high concentration alkaline phenoxide liquors as it occurs in industrial process streams. The total alkali content and total phenol content in samples containing 20–50% (w/v) sodium phenoxide can be directly measured without mutual interference. The first is measured by peak width measurement based FIA with conductimetric detection utilizing an electronic circuit to permit automatic measurement from minima to minima. The total phenol is measured by the Berthelot reaction using NaOCl and ammonia to form indophenol blue, monitored at 660 nm with a light emitting diode-based detector.
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  • 4
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 34 (1988), S. 531-532 
    ISSN: 1432-1041
    Keywords: angina pectoris ; verapamil ; calcium channel blockers ; sustained-release formulation
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Type of Medium: Electronic Resource
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  • 5
    ISSN: 1432-1041
    Keywords: isosorbide 5-mononitrate ; angina pectoris ; asymmetrical dosage timing ; tolerance
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Isosorbide 5-mononitrate is an active metabolite of isosorbide dinitrate and possesses many theoretical advantages over its parent drug. However, the development of partial tolerance has been demonstrated when the drug is given 12 hourly or 8 hourly. We have therefore evaluated the acute and sustained (2 weeks) effects of isosorbide-5-mononitrate 40 mg given twice daily (08.00 h and 14.00 h, allowing an 18-h dose-free period) in 19 patients with stable chronic angina, using computerized exercise testing and a placebo-controlled, double-blind, randomized trial protocol. There were two phases of 2 weeks each in which patients received placebo or active isosorbide-5-mononitrate. Acute testing was performed 2 h after the first dose and chronic testing 2 h after the morning dose on Day 14. Acute testing showed an increase in exercise time from a mean (SD) of 6.7 (2.2) min to 10.1 (2.95) min (P〈0.01) after a single dose of isosorbide-5-mononitrate 40 mg. The time to 1 mm of ST depression, and rest and peak exercise heart rates increased significantly during acute testing with isosorbide-5-mononitrate; resting and peak exercise systolic blood pressures fell significantly. Due to drop outs cross-over analysis was performed on 11 patients who completed both chronic phases and 13 patients were assessed for the comparison of acute isosorbide-5-mononitrate with chronic isosorbide-5-mononitrate. After 2 weeks of therapy exercise time did not show a sustained increase 8.01 (2.14) min chronic placebo to 8.58 (1.93) min chronic isosorbide-5-mononitrate. The improvement in ST segment variables seen acutely was not sustained. These data suggest that the attenuation of the effect of isosorbide-5-mononitrate due to partial tolerance is not mitigated by using an asymmetrical dose regimen.
    Type of Medium: Electronic Resource
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  • 6
    ISSN: 1432-1041
    Keywords: Ranolazine ; angina ; stress testing
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Ranolazine (RS-43285) has been shown to possess significant anti-ischaemic properties in a canine model of reversible myocardial ischaemia. The clinical efficacy of this new agent was assessed by a single blind, placebo controlled study of 14 patients with chronic stable angina. A 2 week placebo phase was followed by therapy with 30 mg and 60 mg of ranolazine tid for 2 weeks each. Graded, symptom limited treadmill exercise tests were performed at the end of each phase, 1.5 h (AM) and 7 h (PM) after the morning dose. An additional exercise test 1.5 h after the first dose of 30 mg was included to assess the acute dose response. In the AM study, the mean exercise time increased from 6.9 min (placebo) to 7.8 min after the first dose of 30 mg and to 8.2 min and 8.5 min respectively at the end of 30 mg and 60 mg phases. In the PM study, exercise time improved from 6.5 min (placebo) to 8.2 min and 7.8 min respectively at the end of 30 mg and 60 mg phases. The time to onset of angina showed a similar improvement. No significant changes were observed in the resting and peak exercise heart rates and blood pressure. This preliminary study suggests that ranolazine may significantly prolong exercise time in patients with stable coronary artery disease without altering heart rates and blood pressure.
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  • 7
    ISSN: 1573-7195
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Description / Table of Contents: Resumé L'insertion d'un dispositif intra-utérin entraîne une réaction inflammatoire persistante qui se manifeste par une augmentation de la dilatation et de la perméabilité vasculaires de l'endomètre exposé au DIU. Les modification inflammatoires provoquées par le dispositif peuvent être maîtrisées par des médicaments anti-inflammatoires. Dans l'étude présentée, effectuée sur des rats, nous signalons que ces changements ont été partiellement enrayés par les anti-inflammatoires suivants, indiqués dans l'ordre de leur efficacité: indométacine, naproxen, ibuprofen. Du point de vue histologique, les dispositifs intra-utérins provoquent une dégénérescence bénigne de l'épithélium utérin et des altérations nécrotiques dans les glandes de l'endomètre. On a également constaté une importante infiltration de leucocytes polymorphonucléaires (PMN) dans le cavité utérine. Il a été partiellement remédié aux changements dégénératifs de l'histoarchitecture épithéliale utérine induits par le dispositif, en administrant un traitement anti-inflammatoire.
    Abstract: Resumen La inserción de un dispositivo intrauterino provoca una reacción inflamatoria persistente que se manifesta por un aumento de la dilatación y de la permeabilidad vasculares del endometrio expuesto al DIU. Los cambios inflamatorios inducidos por el dispositivo pueden ser detenidos mediante el empleo de medicamentos antiinflamatorios. En el presente estudio, realizado en ratas, señalamos que estos cambios fueron parcialmente detenidos con los siguientes antiinflamatorios, indicados por orden de eficacia: indometacina, naproxen, ibuprofen. Desde el punto de vista histológico, los dispositivos intrauterinos provocan una degeneración benigna del epitelio uterino y cambios necróticos en las glándulas del endometrio. Se verificó asimismo una importante infiltración de leucocitos polimorfonucleares (PMN) en la cavidad uterina. Los cambios degenerativos de la histoarquitectura del epitelio uterino inducidos por el dispositivo fueron parcialmente remediados con un tratamiento antiinflamatorio.
    Notes: Abstract Insertion of an IUD causes a persistent inflammatory reaction, evident from an increase in the vascular dilatation and permeability of IUD-exposed endometrium. IUD-induced inflammatory changes can be checked by using anti-inflammatory drugs. In this study in rats, we report that IUD-induced inflammatory changes were partially checked by the use of anti-inflammatory drugs, in order of effectiveness, indomethacin〉naproxen〉ibuprofen. Histologically, IUDs provoke mild degeneration of uterine epithelium and necrotic changes in the endometrial glands. Heavy infiltration of polymorpho-nuclear leukocytes (PMNs) in the uterine lumen was also noticed. IUD-induced degenerative changes in the histoarchitecture of uterine epithelium were partially repaired following treatment with anti-inflammatory drugs.
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  • 8
    Electronic Resource
    Electronic Resource
    Springer
    Pharmaceutical research 16 (1999), S. 1047-1053 
    ISSN: 1573-904X
    Keywords: acromegaly ; somatostatin ; RC-160 ; lipophilization ; GH-inhibitory activity ; protease-resistance
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. Acromegaly is a symptomatically disabling condition, resulting from a growth hormone (GH) secreting pituitary tumor. The somatostatin analog RC-160 is known to potently inhibit hypersecretion of GH, from pituitary adenomas. However, the therapeutic potential of RC-160, is limited by its short serum half life. To overcome this limitation, fatty acids with carbon chain lengths ranging from 4 to 18 were conjugated to RC-160. Methods. The GH-inhibitory activity of these lipopeptides, as well as their binding profile to somatostatin receptors, on the rat pituitary adenoma cell line GH3 was studied in vitro. The relative stability of lipophilized RC-160 towards degradation by crude papaya protease was also determined. Results. The long chain lipopeptides, like myristoyl-RC-160 (carbon chain length = 14) were found to exhibit greater receptor affinity and GH-inhibitory activity, as compared to their counterparts of lower chain lengths. However, the receptor affinity and GH-inhibitory activity of stearoyl-RC-160 (carbon chain length = 18), was found to lower than RC-160 and its lipophilized derivatives. Unlike RC-160, the myristoylated derivative was found to have significantly greater resistance to protease and serum degradation (p 〈 0.01). Conclusions. Lipophilization of RC-160 with long chain fatty acids improves its stability and GH-inhibitory activity. The activity of lipophilized RC-160 seems to increase with increasing hydrophobicity of the lipopeptide, and reaches a maxima at myristoyl-RC-160 for GH3. Hence, optimizing the hydrophobicity should be an important consideration governing the design and synthesis of bioactive lipopeptides.
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  • 9
    ISSN: 1618-2650
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
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