Molecular Pharmacology, Vol 15, 71-77, Copyright © 1979 by the American Society for Pharmacology and Experimental Therapeutics

NMR Study of the Interactions between Flurazepam and Human Serum Albumin

The Nature of the Complexation Site on the Benzodiazepin Molecule

¹ Faculté de Pharmacie Laboratoire de Physique, 27 Bd Jean Moulin 13385, Marseille Cédex 4, France

The nature of the interactions involved in the complexation process between flurazepam and human serum albumin has been investigated by high resolution NMR. The atoms of the flurazepam molecule which make up the site of complexation are identified by proton relaxation rate observations. Calculations show that the association constant of complexation is small (60 M^-1) and it appears that the flurazepam molecules are held tightly in the complex. A term which evaluates the degree of perturbation of each of the protons at the time of complexation is introduced.

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ACKNOWLEDGMENTS We wish to thank M. Dell’Amico and H. Bouteille for their technical assistance.