咖啡因和paraxanthine新陈代谢的差异在人类和小鼠CYP1A2之间。

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Labedzki, Buters J, Jabrane W,富U

咖啡因和paraxanthine新陈代谢的差异在人类和小鼠CYP1A2之间。

生物化学杂志。2002年6月15日,63 (12):2159 - 67。

PubMed ID

12110375 (在PubMed

]

文摘

CYP1A2介导的小鼠模型的描述相比,人类代谢咖啡因的代谢和paraxanthine在人类肝微粒体(LM)(两个样本)和LM CYP1A2-null和野生型老鼠。与喹诺酮抑制实验进行了诺氟沙星和pefloxacin衬底,咖啡因。此外,体内药物动力学CYP1A2-null paraxanthine决心和野生型老鼠。所有产生的主要代谢物LM咖啡因和paraxanthine。在人类LM,咖啡因的主要代谢物paraxanthine (K (M) 0.4和0.5更易与L (1))。在野生型和CYP1A2-null老鼠LM,主要的咖啡因代谢物是1,3,7-trimethylurate,但形成不饱和。paraxanthine形成明显的K (M)从咖啡因在野生型和CYP1A2-null小鼠更易与LM是0.2和4.9 L(1),分别。paraxanthine 1-methylxanthine在人类的主要代谢物(K (M)更易与0.13和0.2 L(1))和野生型老鼠LM (K (0.53 M)更易与L (1))。在CYP1A2-null鼠LM,主要paraxanthine 7-methylxanthine代谢物。喹诺酮类竞争性抑制咖啡因代谢在人类而不是野生型或CYP1A2-null小鼠LM。 No obvious differences were seen for blood pharmacokinetics and urinary metabolite excretion of paraxanthine between CYP1A2-null and wild-type mice. Thus, for paraxanthine, norfloxacin and pefloxacin interaction with CYP1A2 there were clear differences between mice and man. Our results suggest that an interspecies comparison is required for the metabolism of individual xenobiotics interacting with CYP1A2 prior to the use of mice models to predict its toxicity and/or pharmacological activity in man.

beplay体育安全吗DrugBank数据引用了这篇文章

药物酶

药物	酶	类	生物	药理作用	行动
Pefloxacin	细胞色素P450 1 a2	蛋白质	人类	未知的	抑制剂	细节