The classification of drugs on the basis of the drug-binding site on human serum albumin.

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Abstract
The classification of 9 antiinflammatory agents, as well as warfarin and diazepam, on the basis of the binding site on human serum albumin (HSA) was studied by means of competition experiments with bilirubin. The displacement effect was evaluated through kinetic measurements of the free bilirubin concentration by oxidation with hydrogen peroxide and horseradish peroxidase. Bilirubin is a suitable marker for the localization of binding sites, because it has one high-affinity site which is on the loops 3-4 (including Lys-240) in the model of the secondary structure of HSA. Oxyphenbutazone, mefenamic acid and flufenamic acid displaced bilirubin strongly (1st group). Sulfinpyrazone, warfarin, ibuprofen, phenylbutazone and aminopyrine showed moderate effects (2nd group). Ketophenylbutazone, antipyrine and diazepam showed the lowest displacing activity (3rd group). The binding sites of the first group were apparently the same as or very close to the bilirubin site. The 2nd group may be bound in the neighborhood of the bilirubin site or in the overlapping region of the bilirubin and warfarin sites. The 3rd group may be bound to a different site(s) from bilirubin.

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