Determining the best animal model for human cytochrome P450 activities: a comparison of mouse, rat, rabbit, dog, micropig, monkey and man.

作者: J. J. P. Bogaards , M. Bertrand , P. Jackson , M. J. Oudshoorn , R. J. Weaver

DOI: 10.1080/00498250010021684

关键词:

摘要: 1. In the present study, nine cytochrome P450 enzyme activities in seven species were characterized to allow a practical means of comparing this important metabolic step between various test animals and man. 2. Enzyme kinetic parameters first determined towards marker substrates for human enzymes. Inhibition profiles then with both antibodies directed against enzymes chemical inhibitors. 3. Both parameters/enzyme activities, inhibition obtained animal compared those liver microsomes order postulate most similar man regard each individual activity. 4. It was found that, as expected, none tested all measured but that only some could be considered 5. When it is known which are involved metabolism compound, comparative data presented here can used selecting suitable vitro no experiments.

参考文章(52)
Kei Nakachi, Kazue Imai, Kaname Kawajiri, Shin Ichi Hayashi, Polymorphisms of the CYP1A1 and Glutathione S-Transferase Genes Associated with Susceptibility to Lung Cancer in Relation to Cigarette Dose in a Japanese Population Cancer Research. ,vol. 53, pp. 2994- 2999 ,(1993)
Raj Sharma, Brian G. Lake, John Foster, G. Gordon Gibson, Microsomal cytochrome P-452 induction and peroxisome proliferation by hypolipidaemic agents in rat liver. A mechanistic inter-relationship. Biochemical Pharmacology. ,vol. 37, pp. 1193- 1201 ,(1988) , 10.1016/0006-2952(88)90770-8
Victoria A. Eagling, John F. Tjia, David J. Back, Differential selectivity of cytochrome P450 inhibitors against probe substrates in human and rat liver microsomes British Journal of Clinical Pharmacology. ,vol. 45, pp. 107- 114 ,(1998) , 10.1046/J.1365-2125.1998.00679.X
D. J. Newton, R. W. Wang, A. Y. H. Lu, Cytochrome P450 inhibitors. Evaluation of specificities in the in vitrometabolism of therapeutic agents by human liver microsomes. Drug Metabolism and Disposition. ,vol. 23, pp. 154- 158 ,(1995)
E Bush, A Ghosal, P E Thomas, H Satoh, D Moore, Inhibition and kinetics of cytochrome P4503A activity in microsomes from rat, human, and cdna-expressed human cytochrome P450. Drug Metabolism and Disposition. ,vol. 24, pp. 940- 947 ,(1996)
S N Binkley, S A Wrighton, L A Shipley, J E Sharer, M R Vandenbranden, Comparisons of phase I and phase II in vitro hepatic enzyme activities of human, dog, rhesus monkey, and cynomolgus monkey. Drug Metabolism and Disposition. ,vol. 23, pp. 1231- 1241 ,(1995)