抄録
A technique which was designated as"whole-body adsorption autoradiography"was applied to find binding characteristics of bis- and mono-quaternary ammonium ions by rat various tissues. Rat freeze-dried whole-body sections were incubated in an aqueous solution of 14C-labeled deca-, hexa- and dimethonium and tetraethyl- and cetyltrimethylammonium. After rinsing and being freeze-dried, the adsorption of radioactivity was detected by autoradiography. It was found that bisonium ions are highly adsorbed in the cartilage tissues of vertebra, sternum and trachea, wherein a similar high accumulation occurs in vivo, and appreciably adsorbed in the thymus, salivary gland and bone marrow. These adsorptions were interpreted as being due to an ionic bonding of the bis-quaternary ammonium cations to the sulfate and phosphate anions of the chondroitin sulfate and cellular desoxyribonucleic acid (DNA), respectively, probably by forming a bridged structure, with an aid of Alcian Blue staining of the rat whole-body sections (whole-body histochemistry). Close relations between the in vitro adsorption characteristics and the in vivo distribution patterns are pointed out and discussed. It was thus concluded that a physico-chemical binding of a drug molecule to the tissue macromolecules plays an important role in determining the in vivo distribution pattern in animal body and that a combined use of this method with conventional wholebody autoradiography provides a useful tool in establishing the drug distribution characteristics and their interpretation.
