-
- J Helfenbein, C Lartigue, E Noirault, E Azim, J Legailliard, M J Galmier, and J C Madelmont.
- ORPHACHEM, Rue Montalembert, BP 184, 63005 Clermont-Ferrand, France. helfenbein@inserm484.u-clermont1.fr
- J. Med. Chem. 2002 Dec 19;45(26):5806-8.
AbstractThe 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.
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