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Isotopic effect study of propofol deuteration on the metabolism, activity, and toxicity of the anesthetic

…, J Legailliard, MJ Galmier, JC Madelmont

文献索引:Helfenbein; Lartigue; Noirault; Azim; Legailliard; Galmier; Madelmont Journal of Medicinal Chemistry, 2002 , vol. 45, # 26 p. 5806 - 5808

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被引用次数: 31

摘要

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.