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Journal of Pharmacology And Experimental Therapeutics, Vol. 151, Issue 1, 133-138, 1966
Copyright © 1966 by American Society for Pharmacology and Experimental Therapeutics

ENZYME INDUCTION AND INHIBITION IN STUDIES ON THE PHARMACOLOGICAL ACTIONS OF ACETOPHENETIDIN

A. H. Conney 1, M. Sansur 1, F. Soroko 1, R. Koster 1, and J. J. Burns 1

1 The Wellcome Research Laboratories, Burroughs Wellcome & Co. (U.S.A.) Inc., Tuckahoe, New York

Enzyme inhibition by SKF 525-A and enzyme induction by 3-methylcholanthrene can be utilized to investigate whether a drug possesses intrinsic pharmacological activity or whether the drug owes its pharmacological activity to a metabolite. Pretreatment of rats with SKF 525-A inhibits the metabolism of acetophenetidin to N-acetyl-p-aminophenol and increases the antipyretic activity of acetophenetidin. Pretreatment of rats with 3-methylcholanthrene stimulates the metabolism of acetophenetidin to N-acetyl-p-aminophenol and decreases the antipyretic activity of acetophenetidin. These results indicate that acetophenetidin possesses antipyretic activity and that this activity is not dependent on metabolism to N-acetyl-p-aminophenol. Further evidence for this conclusion came from finding that the O-tertiarybutyl and O-trifluoromethyl derivatives of acetophenetidin, which are not O-dealkylated to N-acetyl-p-aminophenol, are more potent and longer lasting antipyretic-analgesic drugs in rats than acetophenetidin.

Accepted on August 12, 1965




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