Abstract

After intravenous injection of three quaternary ammonium derivatives of tropane alkaloid, tritiated p-biphenylmethyl-( dl-tropyl- α-tropinium) bromide ( 3HBTTB), azoniaspiro-(3α-benziloyloxynortropane-8,1-pyrrolidine) chloride ( 3H-ABPC) and 14C-labeled N-methylhyoscine methylsulfate ( 14C-MHM), intracellular distribution of radioactivity was investigated in the liver of rats. Subcellular distribution of 3HBTTB was found to correspond reasonably well to that of acid phosphatase activity, a marker enzyme of lysosomes. The other two drugs were also specific to the light mitochondrial fraction on subcellular distribution. The bulk of the radioactivity in the light mitochondrial fraction was observed to bind to a particulate fraction corresponding in density to the lysosomes. It was found that 3H-BTTB presented in the low density lysosomes of the liver of rats after treatment with RR-2020, a non-ionic detergent, and that the radioactivity bound to the light mitochondrial fraction was solubilized to some extent by the addition in vitro of nonradioactive drugs. These data indicated that the presence of these drugs in the light mitochondrial fraction was due to binding to lysosomal membranes.

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