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Methods for Investigating Affinity and Translocation

The initial evaluation of novel compounds synthesized for targeting a transporter will normally have to be based on the following assays, to get the desired information needed to verify if the compound indeed is a substrate for the transporter and if this results in an increased intestinal permeability  [Pg.248]

Subsequently, in vivo animal studies are necessary to investigate the oral bioavailability. [Pg.248]

During all investigations, stability and metabolism are an issue, especially for prodrugs, which in nature must be biolabile. Today s analytical tools allow a careful analysis of compounds present after the various types of experiments, thus leading to solid interpretations of transporter interactions before going into in vivo studies. [Pg.249]

Quantitative Structure-Activity Relations for Binding of Drug to Transporters [Pg.249]


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Affinity methods

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