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  • 1
    Electronic Resource
    Electronic Resource
    Characterization of the binding of benzodiazepines to human serum albumin (1973)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 280 (1973), S. 229-237 
    Details
    ISSN: 1432-1912
    Keywords: Benzodiazepines ; Albumin Binding ; Gel Filtration
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The binding of eleven benzodiazepine derivatives to human serum albumin (HSA) was determined by means of sephadex gel filtration. The albumin binding of the substances was characterized by the percentage of bound drug, the binding constants k +, K 1 and m, the number of binding sites per albumin molecule, and the free binding energy. Under the conditions chosen in these experiments there seems to exist only one binding site of the same type for all investigated benzodiazepines at the HSA molecule. The affinities of the benzodiazepines to this binding site are very different. It is discussed which part of the benzodiazepine molecule represents the main binding group.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00501348
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    Paper (German National Licenses)
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  • 2
    Electronic Resource
    Electronic Resource
    Influence of pH on the benzodiazepine-human serum albumin complex (1974)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 283 (1974), S. 67-82 
    Details
    ISSN: 1432-1912
    Keywords: Benzodiazepines ; Albumin Binding ; Circular Dichroism ; Gel Filtration ; pH Dependence
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The influence of pH on the binding of benzodiazepine derivatives to HSA was studied by circular dichroism measurements and by gel filtration. The binding of nearly all benzodiazepines is increased by rising the pH from 6.60 to 8.20. For flurazepam, clonazepam, and nitrazepam this increase in binding is due to an increase of the affinities, while for the other substances the affinity remains constant and the number of binding sites is increased from one to two. The changes in binding of the benzodiazepines by rising the pH are explained by a cationic amino acid residue near or at the benzodiazepine binding site of the HSA molecule. This second binding site is not detectable by circular dichroism. For several of the substances rising the pH from 6.60 to 8.20, is accompanied by large alterations of the optical properties of the HSA-benzodiazepine complexes. These alterations are explained by changes of the asymmetric environment of the benzodiazepine binding site at the HSA molecule in the structural transition at slightly alkaline pH values. To explain the different reactions of the benzodiazepines within the N→B transition a theory is given.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00500146
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    Paper (German National Licenses)
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  • 3
    Electronic Resource
    Electronic Resource
    Möglichkeiten zur gezielten Diagnose durch Bestimmung der sauren Desoxyribonucleasen im Urin gesunder Kontrollpersonen und Xeroderma pigmentosum-Patienten (1971)
    Springer
    Journal of molecular medicine 49 (1971), S. 1290-1294 
    Details
    ISSN: 1432-1440
    Keywords: Deoxyribonucleases ; diagnosis ; DNA-damage ; microdiscelectrophoresis ; repairmechanism ; urine ; Xeroderma pigmentosum ; Desoxyribonucleasen ; Diagnose ; DNA-Schaden ; Microdiscelektrophorese ; Repairmechanismus ; Urin ; Xeroderma pigmentosum
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Description / Table of Contents: Zusammenfassung Das Verteilungsmuster der DNase-Aktivität1 im Urin von Normalpersonen und X.p.-Patienten wurde mit einem mikro-disk-elektrophoretischen Verfahren untersucht. Bei saurer Inkubation sind 4 distinkte Aktivitätsbanden im Normalurin nachweisbar. Urin von X.p.-Patienten zeigt eine deutliche Verminderung der 2.–4. Bande, wobei die Veränderung der 3. Bande besonders auffällig ist. Es wurde ferner untersucht, wie sich das Verhalten verändert, wenn statt nativer DNA denaturierte als Substrat angeboten und wenn die zweiwertigen Ionen durch EDTA komplexiert wurden. Eine Aktivitätsverminderung ist nicht auf das Auftreten von Inhibitoren zurückzuführen, sondern wahrscheinlich durch eine Konzentrationsverminderung an Enzym verursacht.
    Notes: Summary The distribution pattern of desoxyribonuclease (DNase) activity1 in the urine of healthy subjects and xeroderma pigmentosum (X.p.) patients has been examined by micro disc electrophoresis. When incubated at pH 5.0, four distinct bands of DNase activity are shown in normal urine. In urine of X.p. patients a significant decrease of the second to fourth band can be observed. The change of the third band is extremely obvious. Further to the influence of native DNA, denaturated DNA and EDTA on the pattern of DNase activities were studied. The decrease of DNase activity in X. p. urine is not due to the presence of an inhibitor but is rather caused by lower enzyme concentrations.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01733085
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    Paper (German National Licenses)
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