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Studies on the pharmacokinetics of bis-quaternary ammonium compounds

III. Autoradiographic studies on the substituent-dependent distribution pattern of 3H-hexamethonium-derivatives in mice

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Summary

On each nitrogen atom of 3H-hexamethonium one methyl group was replaced either by a n-propyl, N-n-propylphthalimide or n-nonyl group. By means of whole-body autoradiography the influence of the different substituents on the distribution pattern was studied in mice after i.v. or s.c. injection. Increasing the chain length of the substituents caused an enhanced accumulation of the respective compounds into secreting tissues, heart muscle, and liver, and an augmentation of biliary excretion. The affinity of the bis-quaternary ammonium compounds for cartilaginous tissues was also altered. The physiological “barriers” between blood and brain or blood and the aqueous humor of the eye, were highly effective against the compounds studied, whereas the placenta could be penetreted by these derivatives.

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Wassermann, O. Studies on the pharmacokinetics of bis-quaternary ammonium compounds. Naunyn-Schmiedeberg's Arch. Pharmacol. 275, 251–261 (1972). https://doi.org/10.1007/BF00500054

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