| Literature DB >> 12477364 |
J Helfenbein1, C Lartigue, E Noirault, E Azim, J Legailliard, M J Galmier, J C Madelmont.
Abstract
The use of isotopic substitution to delay the oxidative metabolism of the anesthetic propofol 1 was studied. The aromatic hydrogens of propofol 1 were replaced by deuterium to produce the mono- and trideuterated derivatives 4 and 5. In vitro metabolic studies on human hepatic microsomes showed no isotopic effect in the para hydroxylation of propofol, and 1, 4, and 5 display similar hypnotic activity and toxicity in mice.Entities:
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Year: 2002 PMID： 12477364 DOI： 10.1021/jm020864q
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446