Isotopic effect study of propofol deuteration on the metabolism,activity, and toxicity of the anesthetic |
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Authors: | Helfenbein J Lartigue C Noirault E Azim E Legailliard J Galmier M J Madelmont J C |
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Institution: | ORPHACHEM, Rue Montalembert, BP 184, 63005 Clermont-Ferrand, France. helfenbein@inserm484.u-clermont1.fr |
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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. |
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