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0090-9556/97/2504-0524-0527$02.00/0
DRUG METABOLISM AND DISPOSITION
Copyright © 1997 by The American Society for Pharmacology and Experimental Therapeutics
Vol. 25, No. 4


SHORT COMMUNICATION
N-Oxygenation of Clozapine by Flavin-Containing Monooxygenase

Meera Tugnait, Edward M. Hawes, Gordon McKay, Allan E. Rettie, Robert L. Haining, and Kamal K. Midha

College of Pharmacy and Nutrition   (M.T., E.M.H., G.M., K.K.M.) University of Saskatchewan   and Department of Medicinal Chemistry   (A.E.R., R.L.H.) University of Washington

The involvement of FMO in the N-oxygenation of CLZ was investigated by use of purified FMOs and human liver microsomes that contained the mean amount of immunoreactive FMO3 relative to other human liver microsomal preparations in a liver bank. In the microsomal preparation the involvement of FMO was indicated through enzyme inhibition by methimazole, heat inactivation, and protection against heat inactivation by NADPH. Also the Michaelis-Menten kinetic constant; KM determined for CLZ N-oxidation catalyzed by purified human FMO3 (324 µM) was very similar to the mean value obtained in these laboratories for the microsomal preparations of seven human livers.

Copyright © 1997 by The American Society for Pharmacology and Experimental Therapeutics


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Copyright © 1997 by the American Society for Pharmacology and Experimental Therapeutics.