With human hair follicles both Phase 1 and Phase 2 activity was detectable in 7 out of 11 subjects. The assay has the advantages of being sensitive, producing single defined metabolites from both Phase 1 and Phase 2 metabolism; is readily adaptable to human skin samples....
药物的代谢通常分为二相:第I相(phase I)生物转化和第Ⅱ相(phase Ⅱ)生物转化。第I相主要是官能团化反应,在酶的催化下对药物分子进行氧化、还原、水解和羟化等反应,在药物分子中引入或使药物分子暴露出极性基团,如羟基、羧基、基和氨基等。第Ⅱ相又称为结合反应,将第【相中药物产生的极性基团与体内的内源性成...
The majority of phase I- and phase II-dependent drug metabolism is carried out by polymorphic enzymes which can cause abolished, quantitatively or qualitat... M Ingelman-Sundberg,C Rodriguez-Antona - 《Philosophical Transactions of the Royal Society B Biological Sciences》 被引量: 158发表: 2005年...
“Phase I and Phase II” Drug Metabolism: Terminology that we Should Phase Out?: Drug Metabolism Reviews: Vol 37, No 4 Click to increase image sizeClick to decrease image size PD Josephy,FP Guengerich - 《Drug Metabolism Reviews》 被引量: 64发表: 2005年 Pharmacokinetics of traditional ...
PCR Array introduction:The Mouse Drug Metabolism Phase II Enzymes RT2 Profiler PCR Array contains 84 genes involved in the enzymatic processes of drug biotransformation. Phase II drug metabolism enzymes catalyze the conjugation of lipophilic compounds with hydrophilic functional groups or moieties to form...
CYP genes are designated in italics (e.g., CYP1A2). The major CYP enzymes in human xenobiotic metabolism are listed in Table 8.3. Also shown are drugs that are known to inhibit CYP enzymes and drugs that increase CYP activity, typically by increasing the amount of enzyme in tissue (...
Human liver microsomal cytochrome P450 mephenytoin 4-hydroxylase, a prototype of genetic polymorphism in oxidative drug metabolism. J Biol Chem 261: 900-921 Two forms of cytochrome P-450 (P-450), designated P-450MP-1 and P-450MP-2, were purified to electrophoretic homogeneity from human liver...
The same limitation holds for PDX models; In vivo models that capture stromal interactions, 3D structure, and drug metabolism. Furthermore, the host mice are immunocompromised to prevent host-graft rejection of the human tumor tissue. Finally, we reason that drug-repurposing designs could benefit ...
The role of CYP2C9 genotype in the metabolism of diclofenac in vivo and in vitro. Eur J Clin Pharmacol 2001;57:729–735. CAS Google Scholar Xie HG, Prasad HC, Kim RB, Stein CM. CYP2C9 allelic variants: ethnic distribution and functional significance. Adv Drug Deliv Rev 2002;54:1257...
13 The proarrhythmic potential of the prodrug terfenadine was revealed at very high doses, however, in patients with liver disease affecting the CYP3A4 enzyme or when patients were taking other medications that inhibited CYP3A410,13,14as this resulte...