PSYCHOACTIVE BUTYROPHENONES - BINDING TO HUMAN AND BOVINE SERUM-ALBUMIN

The binding of psychoactive butyrophenones, moperone, pipamperone, acetabutone, benzperidol, trifluperidol, haloperidol, fluanisone, and droperidol to human and bovine serum albumin was quantitized by means of a fluorescence probe technique. The results indicate that these drugs bind to hydrophobic sites on serum albumin; the association constants, are mainly independent from the albumin source and vary considerably in this class of drugs which has homologous terms, ranging from Ka, 0.17×103M-1 for moperone, to Ka, 1.68×103M-1 for droperidol. Drugs bearing a halogen or methoxy substitution have higher binding values. As the differences in protein binding here reported will be reflected in the pharmacokinetic behaviour of these structurally related drugs they should be considered during therapy. © 1979 The Italian Pharmacological Society.