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Journal of Pharmacology And Experimental Therapeutics, Vol. 149, Issue 3, 436-445, 1965
Copyright © 1965 by American Society for Pharmacology and Experimental Therapeutics

THE METABOLISM OF agr-dl-ACETYLMETHADOL IN THE RAT: THE IDENTIFICATION OF THE PROBABLE ACTIVE METABOLITE

Robert E. McMahon 1, Hilman W. Culp 1, and Frederick J. Marshall 1

1 Lilly Research Laboratories, Indianapolis, Indiana

The major route by which agr-dl-acetylmethadol and agr-dl-noracetylmethadol are metabolized is by enzymatic N-demethylation. The in vivo rate of removal of the first methyl group is roughly three times as great as time rate of removal of the second. Under these conditions the secondary amine, noracetylmethadol, tends to accumulate in body tissue. It is proposed that the active metabolite of agr-l-acetyl-methadol is agr-l-noracetylmethadol and that it is probably responsible for the delayed effects reported by earlier workers.

Ester hydrolysis was also shown to be a significant pathway of metabolism for acetyl-methadol and noracetylmethadol. The corresponding carbinols, however, were not identified in tissues nor found to be excreted in urine or bile.

Acetylmethadol is extensively metabolized in the body. The identity of the ultimate metabolites, which are excreted mainly in bile, is as yet unknown.

Accepted on March 30, 1965




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Copyright © 1965 by the American Society for Pharmacology and Experimental Therapeutics.