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  • 1
    Electronic Resource
    Electronic Resource
    Amsterdam : Elsevier
    Archives of Biochemistry and Biophysics 205 (1980), S. 217-221 
    ISSN: 0003-9861
    Source: Elsevier Journal Backfiles on ScienceDirect 1907 - 2002
    Topics: Biology , Chemistry and Pharmacology , Physics
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Amsterdam : Elsevier
    BBA - Protein Structure 577 (1979), S. 346-359 
    ISSN: 0005-2795
    Keywords: (Human serum albumin) ; Albumin binding ; Benzodiazepine binding site ; Tyrosine residue
    Source: Elsevier Journal Backfiles on ScienceDirect 1907 - 2002
    Topics: Biology
    Type of Medium: Electronic Resource
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  • 3
    Electronic Resource
    Electronic Resource
    Amsterdam : Elsevier
    BBA - Protein Structure 427 (1976), S. 465-480 
    ISSN: 0005-2795
    Source: Elsevier Journal Backfiles on ScienceDirect 1907 - 2002
    Topics: Biology
    Type of Medium: Electronic Resource
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  • 4
    Electronic Resource
    Electronic Resource
    Springer
    Cellular and molecular life sciences 20 (1964), S. 565-566 
    ISSN: 1420-9071
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Summary Δ 5-Pregnen-3,20-dione-N,N'-ethylpyrrolidine-bisguanylhydrazone and Δ5-pregnen-3β-hydroxy-20-one-N,N'-ethyl-pyrrolidine-monoguanylhydrazone inhibit the activity of the ionic pump of cold-stored erythrocytes of guinea-pigs. The contractile force of isolated guinea-pig auricles is decreased by the mono-derivate and increased by the bis-derivate in spite of the similar action upon the pumping mechanism.
    Type of Medium: Electronic Resource
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  • 5
    ISSN: 1432-1912
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Type of Medium: Electronic Resource
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  • 6
    Electronic Resource
    Electronic Resource
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 257 (1967), S. 328-328 
    ISSN: 1432-1912
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Type of Medium: Electronic Resource
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  • 7
    Electronic Resource
    Electronic Resource
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 257 (1967), S. 352-353 
    ISSN: 1432-1912
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Type of Medium: Electronic Resource
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  • 8
    Electronic Resource
    Electronic Resource
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 268 (1971), S. 148-160 
    ISSN: 1432-1912
    Keywords: Digitalislike Acting Substances ; Binding to RNA ; Herzglykosidartig wirkende Substanzen ; Bindung an RNS
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The degree of binding of 3,3′-dimethyl-4,4′-diacetyl-diphenylbisguanylhydrazonedinitrate (BG 60) and of progesterone bisguanylhydrazonedichloride (BG 31) to ribonucleic acid (RNA) was determined by means of equilibrium dialysis and by gel filtration on Sephadex® columns. The interaction of BG 60 and BG 31 and RNA is described by the proportion of the drug bound, the apparent binding constantk +, the constantm, the overall binding constantk 1 and the free energyΔF0. The proportion of BG 60 bound is higher at 4° C than at 22° C. The binding of BG 60 to RNA is only slightly dependent on the pH of the solution, which varied from pH 7.2–8.0. Adding NaCl to the solution reduces the proportion of BG 60 or BG 31 bound to RNA.
    Type of Medium: Electronic Resource
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  • 9
    ISSN: 1432-1912
    Keywords: Isolated Perfused Rat Liver ; Binding to Erythrocytes ; Binding to Albumin ; Phenothiazine Derivatives ; Bisguanylhydrazone
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The binding of lipophilic drugs to albumin and erythrocytes and its importance for the uptake of the drugs into the isolated rat liver were investigated. Promazine and chlorpromazine were taken as lipophilic drugs, which were compared in some experiments with 3,3′-dimethyl-4,4′-diacetyldiphenylbisguanylhydrazone (BG 60), a much more hydrophilic drug. The perfusion medium contained 2% albumin, about 30% bovine erythrocytes and the drug in a concentration of 10−4 M respectively 1.3×l0−4 M in Krebs-Henseleit-solution. In this solution promazine was bound to erythrocytes (69%) and to albumin (20%) whereas the buffer solution contained 11%; 77% of chlorpromazine were bound to erythrocytes, 19% to albumin, whereas the buffer solution contained 4% (Table 1). The distribution of chlorpromazine in the perfusion medium did not depend on the time of incubation (Fig. 1). Increasing the albumin concentration of the perfusion medium caused a rise of the chlorpromazine fraction bound to albumin and a decrease of the fraction bound to the erythrocytes and the fraction of the free, unbound substance (Table 3). The distribution of BG 60 in the perfusion medium markedly depended on the time of incubation. Without incubation 7.5% of BG 60 were bound to erythrocytes, 63% were bound after an incubation time of 2 h (Fig. 1). When suramine was added to the perfusion medium the fraction of promazine bound to albumin increased and the fraction bound to erythrocytes decreased, whereas the fraction of the free substance in the aqueous phase was not significantly changed. In a perfusion medium lacking erythrocytes the fraction of free promazine was considerably higher (Table 1). After the perfusion medium had passed the liver one times, the total chlorpromazine (the fractions of the free and the bound substance) of the first part of the perfusion medium (50 ml) was extracted by the liver (Fig.2). This led to the suggestion that the binding of the phenothiazine derivatives to the membranes of erythrocytes was reversible. In the experiments with BG 60 no fraction of the perfusate of the liver was found, which did not contain BG 60. Beyond that the uptake of BG 60 into the liver depended on the time of incubation of the perfusion medium (Fig. 2). Chlorpromazine was taken up more rapidly than promazine into the recirculating perfused liver (Fig. 3). By suramine the uptake of promazine into the liver was enlarged. KCN did not markedly change the uptake of promazine into the liver (Table 4). If there were no erythrocytes in the perfusion medium the initial uptake of promazine into the liver was increased (Fig.4). There seems to be no difference in the biotransformation of promazine and chlorpromazine as the examination of the perfusate and liver homogenate by thin layer chromatography pointed out. In the experiments with a perfusion medium lacking erythrocytes promazine was much less metabolized (Table 5). The binding of lipophilic substances to erythrocytes may be of similar pharmacokinetic importance as the binding of substances to plasma proteins, as the experiments demonstrated.
    Type of Medium: Electronic Resource
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  • 10
    Electronic Resource
    Electronic Resource
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 258 (1967), S. 288-296 
    ISSN: 1432-1912
    Keywords: Sympathomimetics ; 45Ca-uptake ; Contractility ; Guinea pig auricles ; Sympathomimetica ; 45Ca-Aufnahme ; Kontraktionskraft ; Meerschweinchenvorhöfe
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Description / Table of Contents: Zusammenfassung An isolierten, elektrisch gereizten, linken Meerschweinchenvorhöfen wurden Kontraktionskraft und 45Ca-Aufnahme unter der Einwirkung verschiedener direkt und indirekt wirkender sympathomimetischer Amine gemessen. Alle untersuchten Amine, außer Methoxamin, wirkten positiv inotrop. Die Wirksamkeit von (−)-Adrenalin war etwa 20 mal stärker als die von (+)-Adrenalin, während (−)- und (+)-Synephrin in einem Konzentrationsbereich von 10−7 bis 10−5 g/ml gleich stark wirksam waren. Durch Reserpinvorbehandlung der Tiere konnte die Wirkung von (−)-Synephrin als direkt sympathomimetisch gekennzeichnet werden, die von (+)-Synephrin als vorwiegend indirekt sympathomimetisch. Unter allen Bedingungen zeigte sich eine strenge parallele Beeinflussung von Kontraktionsamplitude und 45Ca-Aufnahme durch alle untersuchten Sympathomimetica. Daraus wird der Schluß gezogen, daß für die positiv inotrope Wirkung der sympathomimetischen Amine eine Erhöhung des Ca-Influx während der Erregung verantwortlich ist.
    Notes: Summary The influence of directly and indirectly acting sympathomimetic amines on contractility and 45Ca-uptake of isolated, electrically driven left guinea pig auricles was investigated. All sympathomimetic amines, except methoxamine, exerted positive inotropic effects. The effect of (-)-adrenaline on contractility was about twenty times stronger than that of (+)-adrenaline, whereas (-)- and (+)-synephrine were equally effective over the concentration range 10−7 to 10−5 g/ml. Depletion of noradrenaline stores by pretreatment of the animals with reserpine greatly reduced the action of (+)-synephrine but not that of (-)-synephrine. It is concluded that (-)-synephrine acts directly sympathomimetically while the effect of (+)-synephrine is mainly an indirect one. Under all conditions employed in this study there was a strongly parallel influence of all sympathomimetic amines investigated on contractility and 45Ca-uptake of isolated guinea pig auricles. Therefore, it is concluded that the increase in Ca-influx during excitation is responsible for the positive inotropic effect of sympathomimetic amines.
    Type of Medium: Electronic Resource
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