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To clarify the mechanism by which basic drugs accumulate in the lung mitochondria, the binding selectivity of drugs to different submitochondrial components of the perfused rat lung was examined. The accumulation of basic drugs was the highest in the mitochondrial outer membrane fraction. The drug accumulation in this fraction increased with lipid solubility and was dose-dependent. It appears then that selective binding sites for basic drugs are present in the mitochondrial outer membrane.

Submitochondrial distribution of basic drugs in the isolated perfused lung.