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Studies on the pharmacokinetics of bis-quaternary ammonium compounds

II. Autoradiographic studies on the distribution of3H-hexamethonium in mice

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Summary

Distribution and accumulation of intravenously and subcutaneously injected tritium-labelled hexamethonium has been studied in mice using autoradiography of whole body sections. The bis-quaternary ammonium compound is rapidly distributed over the organism and excreted mainly by the kidneys, less with the bile. Due to its affinity to “negative binding sites” it combines with acid mucopolysaccharides and is accumulated therefore considerably in connective and cartilaginous tissues. 30 min after either injection route the general distribution pattern of hexamethonium in the organism is characterized as follows (decreasing order): Kidneys, urinary tract, cartilage and connective tissue ≫ lungs > blood, liver > heart and skeletal muscle, gastric and intestinal wall > spleen > adipose tissue, brain and spinal cord.

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A preliminary report of this paper was presented at the 11. Spring Meeting of the German Pharmacological Society, Mainz, Germany, March 1970 (Wassermann, 1970a). Part I: (Wassermann, 1971).

The skilful technical assistence of Mrs. Gisela Kramp is gratefully acknowledged. This work was generously supported by the Fraunhofer-Gesellschaft, Munich.

After completion of the manuscript a paper of Ashgar and Roth (J. Pharmacol.,176, 83–92, 1971) appeared which supports our results presented.

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Wassermann, O. Studies on the pharmacokinetics of bis-quaternary ammonium compounds. Naunyn-Schmiedebergs Arch. Pharmak. 270, 419–427 (1971). https://doi.org/10.1007/BF01002352

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