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RESEARCH PRODUCT

Die Aufnahme von Promazin, Chlorpromazin und deren Desmethylmetaboliten in das isoliert perfundierte Rattenhirn

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The uptake of promazine, chlorpromazine, desmethylpromazine, and desmethylchlorpromazine into the isolated rat brain was determined in relation to their lipophilic character and their binding to albumin and erythroeytes in the perfusion media. The desmethylmetabolites showed about the same degree of binding as their parent compounds promazine and chlorpromazine. On the other hand the partition coefficients of promazine and chlorpromazine were about 10 times higher than those of their desmethylmetabolites. The more hydrophilic desmethyl-metabolites permeated more slowly into the rat brain, but in the distribution equilibrium they may obviously come up to the same concentration in the brain as their parent compounds. In general it was concluded, that the initial uptake of the drugs is influenced by their lipophilic character, whereas the distribution equilibrium depends particularly on their binding in the perfusion media.