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  

Subsequently, in vivo animal studies are necessary to investigate the oral bioavailability. 

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. 

Quantitative Structure-Activity Relations for Binding of Drug to Transporters 

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