van der Graaff M, Vermeulen N P, Hofman P H, Breimer D D
Biochem Pharmacol. 1987 Apr 15;36(8):1321-3. doi: 10.1016/0006-2952(87)90088-8.
Pseudoracemic hexobarbital (HB), consisting of equal molar fractions of S (+) HB and deuterium-labeled R (-) HB, d3 R (-) HB, was administered orally to rats in a dose of 50 mg/kg. Concentrations of both enantiomers in blood were measured by an enantioselective mass fragmentographic assay. Clearance data of S (+) HB and d3 R (-) HB were correlated in untreated rats, and in rats pretreated with 3-methylcholanthrene (MC), carbon tetrachloride (CCl4), and different doses of phenobarbital (PB). Although in the different groups some variation in the clearance ratio of S (+) HB over d3 R (-) HB was found, the clearance of S (+) HB was generally up to a factor of five higher than the clearance of d3 R (-) HB, except for the CCl4-treated rats. From the present data it can be tentatively concluded that S (+) HB and R (-) HB are metabolized by similar (PB-inducible) cytochrome P-450s in control and PB- and MC-pretreated rats and that clearance data obtained with racemic HB following different pretreatments may be employed as a reflection of (PB-inducible) cytochrome P-450 activity.
将由等量摩尔分数的 S(+)己巴比妥（HB）和氘标记的 R(-)己巴比妥（d3 R(-) HB）组成的伪外消旋己巴比妥以 50 mg/kg 的剂量口服给予大鼠。通过对映体选择性质量碎片分析法测定血液中两种对映体的浓度。在未处理的大鼠以及用 3-甲基胆蒽（MC）、四氯化碳（CCl4）和不同剂量苯巴比妥（PB）预处理的大鼠中，对 S(+) HB 和 d3 R(-) HB 的清除率数据进行了相关性分析。尽管在不同组中发现 S(+) HB 与 d3 R(-) HB 的清除率比值存在一些差异，但除 CCl4 处理的大鼠外，S(+) HB 的清除率通常比 d3 R(-) HB 的清除率高至五倍。根据目前的数据可以初步得出结论，在对照以及 PB 和 MC 预处理的大鼠中，S(+) HB 和 R(-) HB 由相似的（PB 可诱导的）细胞色素 P-450 代谢，并且不同预处理后用外消旋 HB 获得的清除率数据可作为（PB 可诱导的）细胞色素 P-450 活性的反映。
