Dvorchik B H, Stenger V G, Hartman R D
Pharmacology. 1979;18(5):241-50. doi: 10.1159/000137259.
Sensitive radiometric assays were adapted to study the development and kinetics of meperidine and methadone N-demethylation and morphine glucuronidation by microsomes isolated from livers of fetal stump-tailed macaques (Macaca arctoides). Times in development selected for study were midterm, three-quarter term, near term and newborn (0.5 h and 14 days). With appropriate attention to keeping blanks low, hepatic drug metabolism was demonstrable as early as midterm. Vmax for the N-demethylation reactions (nmole product/10 min/mg microsomal protein) increased throughout gestation, whereas the apparent Kms remained constant. With respect to morphine glucuronidation, all kinetic parameters remained constant throughout the last half of gestation.
采用灵敏的放射性测定法，研究从胎龄短尾猕猴（熊猴）肝脏分离的微粒体对哌替啶和美沙酮N-去甲基化以及吗啡葡萄糖醛酸化的发生发展及动力学。选取研究的发育阶段为中期、孕晚期、接近足月和新生期（0.5小时和14天）。在适当注意保持空白值较低的情况下，早在中期就可证实肝脏药物代谢。整个妊娠期，N-去甲基化反应的最大反应速度（纳摩尔产物/10分钟/毫克微粒体蛋白）增加，而表观米氏常数保持不变。关于吗啡葡萄糖醛酸化，在妊娠后半期所有动力学参数均保持不变。
