DMD # 4242 1 Importance of CYP 2 D 3 in polymorphism of diazepam p - hydroxylation in rats
نویسندگان
چکیده
منابع مشابه
Importance of CYP2D3 in polymorphism of diazepam p-hydroxylation in rats.
Diazepam was metabolized to three primary metabolites, 3-hydroxy-diazepam, N-desmethyl-diazepam, and p-hydroxy-diazepam. Our previous studies reported metabolic position-specific inter- or intrastrain differences in diazepam metabolism among Sprague-Dawley, Brown Norway, Dark Agouti, and Wistar rats. Especially, there were marked ( approximately 300 fold) inter- or intrastrain differences in di...
متن کاملGenetic basis of inter- and intrastrain differences in diazepam p-hydroxylation in rats.
Diazepam (7-chloro-1,3-dihydro-1-methyl-5-phenyl-2H-1,4-benzodiazepin-2-one) is widely used as a sedative, hypnotic, and anti-anxiety drug. At low diazepam concentrations, p-hydroxylation is the major metabolic pathway in rat liver microsomes. However, there are marked ( approximately 300-fold) inter- and intrastrain differences in the activity among Sprague-Dawley, Brown Norway, Dark Agouti, a...
متن کاملStrain differences in diazepam metabolism at its three metabolic sites in sprague-dawley, brown norway, dark agouti, and wistar strain rats.
Knowledge of strain differences in drug metabolism is important for the selection of animals for pharmacokinetic, pharmacodynamic, and toxicological studies. Hepatic microsomes from Sprague-Dawley (SD) and Brown Norway (BN) rats had 300-fold higher diazepam p-hydroxylation activity than Dark Agouti (DA) and Wistar (W) rats at a low diazepam concentration (3 microM). Kinetic studies indicated th...
متن کاملDMD #30866 1 Relevance of non-synonymous CYP2C8 polymorphisms to 13-cis retinoic acid and paclitaxel hydroxylation
word count: 215 Introduction word count: 414 Results and Discussion word count: 1,010 Abreviations: CYP, Cytochrome P450; 13cisRA, 13-cis retinoic acid; LCMS, Liquid chromatography-mass spectrometry. This article has not been copyedited and formatted. The final version may differ from this version. DMD Fast Forward. Published on April 26, 2010 as DOI: 10.1124/dmd.109.030866 at A PE T Jornals on...
متن کاملRole of a potent inhibitory monoclonal antibody to cytochrome P-450 3A4 in assessment of human drug metabolism.
Cytochrome P-450 (CYP) 3A4 is an inordinately important CYP enzyme that catalyzes the metabolism of a vast array of clinically used drugs. Microsomal proteins of Spodoptera frugiperda (Sf21) insect cells infected with recombinant baculoviruses encoding CYP3A4 cDNA were used to immunize mice and to develop a monoclonal antibody (mAb(3A4a)) specific to CYP3A4 through the use of hybridoma technolo...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
عنوان ژورنال:
دوره شماره
صفحات -
تاریخ انتشار 2005