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  • 1
    Electronic Resource
    Electronic Resource
    Blut-Hirnschranke und Penetration von Zytostatika (1985)
    Springer
    Journal of molecular medicine 63 (1985), S. 565-571 
    Details
    ISSN: 1432-1440
    Keywords: Blood-brain barrier ; Drug transfer ; Alkylglycerols
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The penetration of 12 commonly used anticancer agents through the blood-brain barrier (BBB) was measured in a rat model using a single-injection tissue-sampling technique. Two of the tested drugs penetrated the barrier, but only to a limited extent. Entry of the drugs into the brain tissue critically depends on molecular weight and lipophilia of the respective test compound. For drugs with a molecular weight of less than 500, BBB simply behaves like an oil/water interphase, whereas drugs with a molecular weight greater than 500 are practically excluded from transport through the BBB even if they show a favourable oil/water partition coefficient. However, permeability of cytostatics was strongly increased if short chain alkylglycerols, up to final concentrations of about 0.3 mol/l were added to the injected solution. Under these conditions the Brain-Uptake-Index (BUI) reached values up to about 50% (cyclophosphamide), depending on lipid solubility and molecular dimension of the respective test compound and the alkyl chain length of the glycerol derivative.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01733202
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    Paper (German National Licenses)
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  • 2
    Electronic Resource
    Electronic Resource
    Effect of ether lipids of mousé granulocyte-macrophage progenitor cells (1989)
    Springer
    Cancer chemotherapy and pharmacology 24 (1989), S. 58-60 
    Details
    ISSN: 1432-0843
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary In this study we determined the potential bone marrow toxicity of the ether lipid derivatives 1-0-octadecyl-2-0-methyl-rac-glycero-3-phosphocholine (OcMe-G-3-PC), 1-0-hexadecyl-propanediol-2-phosphocholine (He-Pr-2-PC), and hexadecylphosphocholine (He-PC). OcMe-G-3-PC inhibited the proliferation of mouse granulocytemacrophage progenitor cells (GM-CFCs) at a dose of 1 μg/ml, whereas He-Pr-2-PC and He-PC started to inhibit the growth of hemopoietic precursors at 5 μg/ml. In contrast to this finding, NMRI mice given 10 mg/kg i.v. daily for 4 weeks and 20 or 30 mg/kg for 5 days showed no bone marrow toxicity. We conclude that the dose-dependent toxic effects observed in vitro are within the physiological tolerance in vivo.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00254107
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    Paper (German National Licenses)
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  • 3
    Electronic Resource
    Electronic Resource
    Brain uptake and CNS levels of 1-(2-chloroethyl)-1-nitroso-3-(2-hydroxyethyl)urea (HECNU) (1987)
    Springer
    Investigational new drugs 5 (1987), S. 361-364 
    Details
    ISSN: 1573-0646
    Keywords: 1-(2-chloroethyl)-1-nitroso-3(2-hydroxyethyl)urea (HECNU) ; blood brain barrier ; cerebrospinal fluid concentration
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Abstract The uptake of 14C-labeled 1-(2-chloroethyl)-1-nitroso-3-(2-hydroxyethyl) urea (HECNU) into the brain was investigated in the rat after intracarotid injection according to the method of OLDENDORF, as well as in cisternal cerebrospinal fluid obtained by suboccipital puncture after i.v. injection of the drug. The brain uptake index was 31.9 ± 2.9%. Cerebrospinal fluid/blood quotients after i.v. injection were 0.82 at 10 min and 1.10 at 60 min. The results of both methods clearly show that HECNU, in spite of its hydrophilic property, easily penetrates the blood-brain barrier.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00169975
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    Paper (German National Licenses)
    Fulltext
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