PT  - JOURNAL ARTICLE
AU  - Maohe Yan
AU  - Leslie T. Webster, Jr.
AU  - Jeffrey L. Blumer
TI  - 3-<em>O</em>-Methyldobutamine, a Major Metabolite of Dobutamine in Humans
AID  - 10.1124/dmd.30.5.519
DP  - 2002 May 01
TA  - Drug Metabolism and Disposition
PG  - 519--524
VI  - 30
IP  - 5
4099  - http://dmd.aspetjournals.org/content/30/5/519.short
4100  - http://dmd.aspetjournals.org/content/30/5/519.full
SO  - Drug Metab Dispos2002 May 01; 30
AB  - Dobutamine is a synthetic ionotropic catecholamine commonly used to treat heart failure and shock. The catabolic fate of dobutamine in humans has yet to be reported, although formation of 3-O-methyldobutamine represents the principal pathway of dobutamine disposition in the dog. Herein, we describe the isolation and identification of 3-O-methyldobutamine in the urine of children receiving infusions of racemic dobutamine. In a 9-year-old child with heart failure ∼80% of dobutamine administered intravenously at steady state was detected in the urine. Forty-seven percent of infused dobutamine was identified as 3-O-methyldobutamine and its acid-hydrolyzed derivatives, the latter mostly conjugated with sulfate (33%). Thirty-two percent consisted of acid-hydrolyzed dobutamine metabolites, primarily conjugated with sulfate (16%). Sonicates of human blood mononuclear cells catalyzed the formation of 3-O-methyldobutamine from dobutamine andS-adenosylmethionine in vitro. These findings indicate that formation of 3-O-methyldobutamine constitutes a major pathway of dobutamine metabolism in humans. The American Society for Pharmacology and Experimental Therapeutics