• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利：CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验

Diazepam metabolism by rat and human liver in vitro: inhibition by mephenytoin.

作者信息

Beischlag T V, Kalow W, Mahon W A, Inaba T

机构信息

Department of Pharmacology, University of Toronto, Canada.

出版信息

Xenobiotica. 1992 May;22(5):559-67. doi: 10.3109/00498259209053119.

DOI:10.3109/00498259209053119
PMID:1413871
Abstract
  1. Diazepam metabolism and its association with mephenytoin hydroxylase were studied in vitro using human and rat livers. 2. Enzyme kinetic parameters were obtained for the formation of p-hydroxydiazepam (p-hydroxy-DZP), N-desmethyldiazepam (NDZ), and temazepam (TMZ) from diazepam (DZP) in rat liver fractions. The Km values for formation in rat of p-hydroxy-DZP, NDZ and TMZ were 14 +/- 3 (SEM) microM, 44 +/- 4 and 63 +/- 8, respectively; clearance values calculated from Vmax/Km were 5.7, 3.2 and 4.9 ml/g per min, respectively. 3. Mephenytoin (MP) competitively inhibited, in rat liver, the formation of NDZ, but not the formation of p-hydroxy-DZP or TMZ; in human liver neither NDZ nor TMZ formation was inhibited by MP. 4. In seven different human livers the formation of p-hydroxy-DZP represented a minor pathway compared to the formation of NDZ and TMZ.
摘要

相似文献

1
Diazepam metabolism by rat and human liver in vitro: inhibition by mephenytoin.
Xenobiotica. 1992 May;22(5):559-67. doi: 10.3109/00498259209053119.
2
Metabolism of diazepam in vitro by human liver. Independent variability of N-demethylation and C3-hydroxylation.地西泮在人肝脏中的体外代谢。N-去甲基化和C3-羟基化的独立变异性。
Drug Metab Dispos. 1988 Jul-Aug;16(4):605-8.
3
Diazepam metabolism by human liver microsomes is mediated by both S-mephenytoin hydroxylase and CYP3A isoforms.人肝微粒体对安定的代谢由S-美芬妥英羟化酶和CYP3A同工酶介导。
Br J Clin Pharmacol. 1994 Aug;38(2):131-7. doi: 10.1111/j.1365-2125.1994.tb04336.x.
4
Cytochrome P450IIIA enzymes in rat liver microsomes: involvement in C3-hydroxylation of diazepam and nordazepam but not N-dealkylation of diazepam and temazepam.大鼠肝微粒体中的细胞色素P450IIIA酶：参与地西泮和去甲地西泮的C3-羟基化反应，但不参与地西泮和替马西泮的N-脱烷基反应。
Mol Pharmacol. 1990 May;37(5):767-74.
5
Characterization of equine cytochrome P450: role of CYP3A in the metabolism of diazepam.马细胞色素P450的特性：CYP3A在安定代谢中的作用。
J Vet Pharmacol Ther. 2016 Oct;39(5):478-87. doi: 10.1111/jvp.12303. Epub 2016 Mar 11.
6
Role of cDNA-expressed human cytochromes P450 in the metabolism of diazepam.互补脱氧核糖核酸表达的人细胞色素P450在地西泮代谢中的作用。
Biochem Pharmacol. 1998 Mar 15;55(6):889-96. doi: 10.1016/s0006-2952(97)00558-3.
7
Inhibition of diazepam metabolism in microsomal- and perfused liver preparations of the rat by desmethyldiazepam, N-methyloxazepam and oxazepam.去甲西泮、N-甲基奥沙西泮和奥沙西泮对大鼠微粒体和灌注肝制剂中地西泮代谢的抑制作用。
Eur J Drug Metab Pharmacokinet. 1985 Jan-Mar;10(1):15-20. doi: 10.1007/BF03189692.
8
Concentration-dependent metabolism of diazepam in mouse liver.地西泮在小鼠肝脏中的浓度依赖性代谢。
J Pharmacokinet Biopharm. 1995 Jun;23(3):243-66. doi: 10.1007/BF02354284.
9
Strain differences in diazepam metabolism at its three metabolic sites in sprague-dawley, brown norway, dark agouti, and wistar strain rats.地西泮在斯普拉格-道利、棕色挪威、黑豚鼠和Wistar品系大鼠的三个代谢位点的代谢存在品系差异。
Drug Metab Dispos. 2004 Sep;32(9):959-65.
10
Importance of genetic factors in the regulation of diazepam metabolism: relationship to S-mephenytoin, but not debrisoquin, hydroxylation phenotype.遗传因素在地西泮代谢调节中的重要性：与S-美芬妥因而非异喹胍羟化表型的关系。
Clin Pharmacol Ther. 1989 Apr;45(4):348-55. doi: 10.1038/clpt.1989.40.

引用本文的文献

1
Concentration-dependent metabolism of diazepam in mouse liver.地西泮在小鼠肝脏中的浓度依赖性代谢。
J Pharmacokinet Biopharm. 1995 Jun;23(3):243-66. doi: 10.1007/BF02354284.
2
Diazepam metabolism by human liver microsomes is mediated by both S-mephenytoin hydroxylase and CYP3A isoforms.人肝微粒体对安定的代谢由S-美芬妥英羟化酶和CYP3A同工酶介导。
Br J Clin Pharmacol. 1994 Aug;38(2):131-7. doi: 10.1111/j.1365-2125.1994.tb04336.x.