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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    Pharmaceutical research 4 (1987), S. 142-146 
    ISSN: 1573-904X
    Keywords: basic drug ; lipid solubility ; lung ; mitochondria ; drug binding to lung mitochondria
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The role of the mitochondria in the accumulation of basic amine drugs in the rat lung was studied. Drug binding to the mitochondria was rapid and reached maximum levels after 2.5 min of incubation. Lipophilic basic drugs accumulated in the mitochondria more than nonlipophilic basic drugs and non-basic drugs, and the accumulation was dose dependent. Schatchard plots revealed at least two independent sets of binding sites for basic drugs in the mitochondria. The binding was competitively inhibited by other basic drugs but not nonbasic drugs. The degree of inhibition by competing basic drugs was correlated with their lipid solubilities. These findings with isolated mitochondria agree with previous results obtained with the perfused lung preparation and indicate that the mitochondria play an important role in the accumulation of basic drugs in the lung.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    Pharmaceutical research 4 (1987), S. 50-53 
    ISSN: 1573-904X
    Keywords: basic drug ; lipid solubility ; lung ; mitochondria ; subcellular fractionation
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract To clarify the mechanism by which basic drugs accumulate in the lung, the binding selectivity of drugs to different subcellular structures of the perfused rat lung was examined. Imipramine, quinine, and metoclopramide were used as examples of basic drugs. The accumulation of basic drugs was highest in the mitochondrial fraction. The drug accumulation in the lung mitochondrial fraction increased with increasing lipid solubility and was dose dependent. These results suggest the presence of specific binding sites for basic drugs in mitochondria and that mitochondria play an important role as a reservoir for basic drugs.
    Type of Medium: Electronic Resource
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