Abstract

St-155 [2-(2,6-dichloroanilino)-2-imidazoline] is a new hypotensive agent effective in microgram doses. The physiological disposition of the compound in the rat was examined by using 14C-labeled drug and a selective extraction procedure. St-155 was found to be localized reversibly in all of the tissues examined, but especially in the submaxillary gland. The gland to plasma concentration ratio was about 40. The concentration in saliva was lower than that for the plasma, indicating that the compound had accumulated in the gland itself. Examination of the uptake of St-155 into sub-maxillary slices in vitro showed that the accumulation reflected the concentration of non-ionized compound in the bath fluid, suggesting that passage of the drug from plasma to saliva occurs by diffusion of this form of St-155 through the gland.

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