立体选择glucuronidation和羟基化etodolac UGT1A9和CYP2C9的男人。

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Tougou K, Gotou H, Ohno Y,中村

立体选择glucuronidation和羟基化etodolac UGT1A9和CYP2C9的男人。

Xenobiotica。2004年5月,34 (5):449 - 61。doi: 10.1080 / 00498250410001691280。

PubMed ID

15370961 (在PubMed

]

文摘

1。体外代谢研究etodolac进行。S -和R-etodolac转化为acylglucuronide和羟化代谢产物UDP-glucuronosyltransferase (UGT)和细胞色素P450在微粒体。然而,UGT和P450的同分异构体的立体选择性是相反的。S-etodolac比R-etodolac的UGT glucuronidated优先。相比之下,R-etodolac被P450比S-etodolac羟化优先。2。最大的几个人类P450酶,CYP2C9 R-etodolac羟基化的活动。Sulfaphenazole、CYP2C9抑制剂和anti-CYP2C9抗体抑制R-etodolac羟基化的人类肝脏微粒体。CYP2C9因此导致R-etodolac的立体选择羟基化。 3. Of several human UGT enzymes, UGT1A9 had the greatest activity for glucuronidation of S-etodolac. Propofol and thyroxine, inhibitors of UGT1A9, inhibited the glucuronidation of S-etodolac in human liver microsomes. Therefore, UGT1A9 is mainly responsible for the stereoselective glucuronidation of S-etodolac. 4. Because S-etodolac was metabolized more rapidly than R-etodolac in human cryopreserved hepatocytes, the stereoselectivities of UGT1A9 for etodolac substantially influenced the overall metabolism of S- and R-etodolac in man.

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
Etodolac	细胞色素P450 2 c9	蛋白质	人类	未知的	底物	细节