Hepatic transport of organic cations: Active uptake of a quaternary ammonium compound, procaine amide ethobromide (cas 17010-70-7), by rat liver slices

Add time:08/07/2019    Source:sciencedirect.com

When rat liver slices were incubated aerobically at 37 with procaine amide ethobromide (PAEB), the compound readily entered the tissue and attained a concentration in tissue water about three times that in the suspending medium. Accumulation of PAEB in the slices occurred by a process that became saturated at high concentrations of the drug. In addition, accumulation was prevented by anaerobic conditions, by metabolic inhibitors such as iodoacetate or 2,4-dinitrophenol, and by certain quaternary amine compounds which presumably compete with PAEB for the uptake process. PAEB was bound to a small extent in homogenates of liver, but the characteristics of the binding were such that the binding could not account for the bulk of the accumulation of drug seen in tissue slices. It appears that the drug is accumulated by liver slices by an active transport process, and that this process is closely related to the secretory process for the biliary excretion of PAEB and certain other quaternary ammonium ions in the living animal.

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