Interaction of the antimalarial alpha-dibutylaminomethyl-2,6-bis(trifluoromethylphenyl)-4-pyridinemethanol with human serum albumin.

O J Bouwsma, J T Stewart, J J Vallner

Journal of pharmaceutical sciences 1979 Jan

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Binding of the antimalarial alpha-dibutylaminomethyl-2,6-bis(trifluoromethylphenyl)-4-pyridinemethanol with human serum albumin was studied using difference spectroscopy, fluorescence quenching, and equilibrium dialysis. Results indicated that the number of high affinity binding sites of the drug on protein is 0.45, with the total number of binding sites being 3.3--4.0. The binding constants were in the range of 0.57--4.00 x 10(6) M-1. The drug was bound more strongly to a nonionic detergent than to either a cationic or anionic detergent. Interpretation of these data and fluorescence quenching results indicated that the drug is possibly bound to a hydrophobic site on human serum albumin.

Citation

O J Bouwsma, J T Stewart, J J Vallner. Interaction of the antimalarial alpha-dibutylaminomethyl-2,6-bis(trifluoromethylphenyl)-4-pyridinemethanol with human serum albumin. Journal of pharmaceutical sciences. 1979 Jan;68(1):45-8