Billings R E, McMahon R E, Ashmore J, Wagle S R
Drug Metab Dispos. 1977 Nov-Dec;5(6):518-26.
The metabolism of drugs in isolated rat hepatocytes has been investigated. Drugs which are metabolized by aromatic hydrolation, aliphatic hydroylation, N-demethylation, or glucuronidation have been used as substrates. With some substrates the rate of metabolism in isolated hepatocytes compares with that in hepatic 900g supernatant fraction or microsomes, but other substrates are metabolized at a slower rate in isolated hepatocytes. For example, the rate of butamoxane hydroxylation in isolated hepatocytes is slower than that in microsomes. However, the rate of hydroxylation is hepatocytes is identical to that in perfused liver. The metabolism of drugs in isolated hepatocytes correlates with in vivo drug metabolism better than does metabolism in the hepatic 9000g supernatant fraction or microsomes.
已对分离的大鼠肝细胞中药物的代谢进行了研究。通过芳香族羟化、脂肪族羟化、N-脱甲基或葡萄糖醛酸化代谢的药物已被用作底物。对于一些底物，分离的肝细胞中的代谢速率与肝900g上清液部分或微粒体中的代谢速率相当，但其他底物在分离的肝细胞中的代谢速率较慢。例如，分离的肝细胞中布他莫烷的羟化速率比微粒体中的慢。然而，肝细胞中的羟化速率与灌注肝脏中的相同。分离的肝细胞中药物的代谢与体内药物代谢的相关性比肝9000g上清液部分或微粒体中的代谢更好。
