体内的H2受体阻滞剂,西咪替丁、雷尼替丁、减少细胞色素的内容P450IID (CYP2D)在大鼠肝微粒体亚科和他们的活动。

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西冈Orishiki M,松尾Y, M,川Y

体内的H2受体阻滞剂,西咪替丁、雷尼替丁、减少细胞色素的内容P450IID (CYP2D)在大鼠肝微粒体亚科和他们的活动。

Int。1994 6月,26 (6):751 - 8。

PubMed ID

8063004 (在PubMed

]

文摘

1。体内的影响政府的H2受体阻滞剂,西咪替丁、雷尼替丁(0.6更易/公斤体重/天,5天),在几个P450酶同功酶,在P450IID (CYP2D)亚科,及其在大鼠肝微粒体单氧酶活动调查。2。体内的西咪替丁、雷尼替丁P450酶同功酶的内容和活动减少P450-linked单氧酶系统;即。,benzphetamine N-demethylase,氨基比林N-demethylase, 7-ethoxycoumarin O-deethylase, debrisoquine 4-hydroxylase bufuralol 1羟化酶。3所示。酶的抑制作用的活动P450IID (CYP2D)与单氧酶系统研究了免疫印迹分析血清含有anti-CYP2D6免疫球蛋白,即。,LKM1自身抗体。P450IID的数量(CYP2D)在肝微粒体下降更显著的组管理雷尼替丁或西咪替丁体内比控制。4所示。 The effects of cimetidine and ranitidine on the activities of the P450IID (CYP2D)-linked monooxygenase systems were investigated in vitro. The activities of debrisoquine 4-hydroxylase and bufuralol 1'-hydroxylase were inhibited in vitro by cimetidine or ranitidine at a higher concentration than that on in vivo administration of either H2 blocker. 5. The kinetic parameters for cimetidine or ranitidine as to the activities of debrisoquine 4-hydroxylase and bufuralol 1'-hydroxylase in liver microsomes were determined by means of Lineweaver-Burk plots. 6. The suppressive effects of cimetidine and ranitidine on the activities of P450IID (CYP2D)-linked monooxygenase systems in vivo were found to be due to a decrease of the content of the P450IID (CYP2D) protein.

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
西咪替丁	细胞色素P450 2 d6	蛋白质	人类	未知的	抑制剂	细节