Kammerer R C, Schmitz D A
Xenobiotica. 1986 Jul;16(7):681-90. doi: 10.3109/00498258609043558.
Metabolism of lidocaine in rabbit liver 9000 g supernatant fraction was examined. A capillary g.l.c. assay was developed to separate seven known metabolites of lidocaine, and all seven metabolites were identified in extracts of incubations of lidocaine with rabbit-liver fractions. These metabolites were monoethylglycinexylidide(I), glycinexylidide(II), 3-hydroxymonoethylglycinexylidide(III), 3-hydroxylidocaine(IV), 4-hydroxylidocaine(V), xylidine(VI) and 4-hydroxyxylidine(VII). A new metabolite, 2-amino-3-methylbenzoic acid(VIII), was identified in extracts of incubations of lidocaine with rabbit-liver fractions, by comparison of the mass-spectral fragmentation patterns and g.l.c. retention time with those of the authentic compound. The formation of VIII is dependent on protein, NADPH, time, O2, and the presence of soluble enzymes. Quantitative analysis of metabolites I-VIII after a two hour incubation accounts for 89% of the metabolized lidocaine.
研究了利多卡因在兔肝9000g上清液组分中的代谢情况。开发了一种毛细管气相色谱分析法来分离利多卡因的七种已知代谢物，并且在利多卡因与兔肝组分孵育的提取物中鉴定出了所有七种代谢物。这些代谢物分别是单乙基甘氨酸酰基苯胺（I）、甘氨酸酰基苯胺（II）、3-羟基单乙基甘氨酸酰基苯胺（III）、3-羟基利多卡因（IV）、4-羟基利多卡因（V）、二甲苯胺（VI）和4-羟基二甲苯胺（VII）。通过将质谱裂解模式和气相色谱保留时间与 authentic 化合物进行比较，在利多卡因与兔肝组分孵育的提取物中鉴定出一种新的代谢物2-氨基-3-甲基苯甲酸（VIII）。VIII的形成取决于蛋白质、NADPH、时间、O2以及可溶性酶的存在。孵育两小时后对代谢物I-VIII进行定量分析，结果表明其占代谢掉的利多卡因的89%。
