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Characterization of the binding of benzodiazepines to human serum albumin

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Summary

The binding of eleven benzodiazepine derivatives to human serum albumin (HSA) was determined by means of sephadex gel filtration.

The albumin binding of the substances was characterized by the percentage of bound drug, the binding constants k +, K 1 and m, the number of binding sites per albumin molecule, and the free binding energy. Under the conditions chosen in these experiments there seems to exist only one binding site of the same type for all investigated benzodiazepines at the HSA molecule. The affinities of the benzodiazepines to this binding site are very different. It is discussed which part of the benzodiazepine molecule represents the main binding group.

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Müller, W., Wollert, U. Characterization of the binding of benzodiazepines to human serum albumin. Naunyn-Schmiedeberg's Arch. Pharmacol. 280, 229–237 (1973). https://doi.org/10.1007/BF00501348

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