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一种通过抑制研究鉴定为司巴丁-异喹胍单加氧酶的人细胞色素P-450。

A human cytochrome P-450 characterized by inhibition studies as the sparteine-debrisoquine monooxygenase.

作者信息

Inaba T, Nakano M, Otton S V, Mahon W A, Kalow W

出版信息

Can J Physiol Pharmacol. 1984 Jul;62(7):860-2. doi: 10.1139/y84-144.

DOI:10.1139/y84-144
PMID:6498616
Abstract

The present study compares the debrisoquine monooxygenase and the sparteine monooxygenase activities of human liver microsomes. In the presence of 14 competitive inhibitors, apparent inhibition constants (Ki) as determined by these two activities ranged over four orders of magnitude with a correlation coefficient 0.99. These in vitro results represent the strongest evidence to date that the debrisoquine monooxygenase and the sparteine monooxygenase are identical and involve a single isozyme of cytochrome P-450.

摘要

本研究比较了人肝微粒体中异喹胍单加氧酶和司巴丁单加氧酶的活性。在14种竞争性抑制剂存在的情况下,由这两种活性所测定的表观抑制常数(Ki)范围跨越四个数量级,相关系数为0.99。这些体外实验结果是迄今为止最有力的证据,表明异喹胍单加氧酶和司巴丁单加氧酶是相同的,且涉及细胞色素P - 450的单一同工酶。

相似文献

1
A human cytochrome P-450 characterized by inhibition studies as the sparteine-debrisoquine monooxygenase.一种通过抑制研究鉴定为司巴丁-异喹胍单加氧酶的人细胞色素P-450。
Can J Physiol Pharmacol. 1984 Jul;62(7):860-2. doi: 10.1139/y84-144.
2
In vitro evidence against the oxidation of quinidine by the sparteine/debrisoquine monooxygenase of human liver.关于人肝脏中司巴丁/异喹胍单加氧酶对奎尼丁氧化作用的体外证据。
Drug Metab Dispos. 1988 Jan-Feb;16(1):15-7.
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Substrate specificity of the form of cytochrome P-450 catalyzing the 4-hydroxylation of debrisoquine in man.人肝脏中催化异喹胍4-羟化反应的细胞色素P-450形式的底物特异性
Mol Pharmacol. 1983 Mar;23(2):474-81.
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Xenobiotic and endobiotic inhibitors of cytochrome P-450dbl function, the target of the debrisoquine/sparteine type polymorphism.
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Debrisoquine/sparteine-type polymorphism of drug oxidation. Purification and characterization of two functionally different human liver cytochrome P-450 isozymes involved in impaired hydroxylation of the prototype substrate bufuralol.药物氧化的异喹胍/鹰爪豆碱型多态性。参与原型底物布呋洛尔羟化受损的两种功能不同的人肝细胞色素P-450同工酶的纯化与特性鉴定。
J Biol Chem. 1986 Sep 5;261(25):11734-43.
6
Enzymatic basis of the debrisoquine/sparteine-type genetic polymorphism of drug oxidation. Characterization of bufuralol 1'-hydroxylation in liver microsomes of in vivo phenotyped carriers of the genetic deficiency.药物氧化的去甲丙咪嗪/鹰爪豆碱型遗传多态性的酶学基础。对遗传缺陷的体内表型携带者肝脏微粒体中布呋洛尔1'-羟化作用的表征。
Biochem Pharmacol. 1987 Dec 1;36(23):4145-52. doi: 10.1016/0006-2952(87)90573-9.
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Evidence in humans for variant allozymes of the nondeficient sparteine/debrisoquine monooxygenase (P45OIID 1) in vitro.
Drug Metab Dispos. 1989 May-Jun;17(3):334-40.
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Interactions of bupranolol with the polymorphic debrisoquine/sparteine monooxygenase (CYP2D6).
Eur J Clin Pharmacol. 1993;45(3):261-4. doi: 10.1007/BF00315393.
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Impairment of debrisoquine 4-hydroxylase and related monooxygenase activities in the rat following treatment with propranolol.普萘洛尔治疗后大鼠异喹胍4-羟化酶及相关单加氧酶活性受损。
Biochem Pharmacol. 1991;41(6-7):861-5. doi: 10.1016/0006-2952(91)90189-c.
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Characterization of a human liver cytochrome P-450 involved in the oxidation of debrisoquine and other drugs by using antibodies raised to the analogous rat enzyme.通过使用针对类似大鼠酶产生的抗体来鉴定参与异喹胍和其他药物氧化的人肝脏细胞色素P-450。
Proc Natl Acad Sci U S A. 1984 Dec;81(23):7348-52. doi: 10.1073/pnas.81.23.7348.

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Clin Pharmacokinet. 1986 Jan-Feb;11(1):1-17. doi: 10.2165/00003088-198611010-00001.
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Br J Clin Pharmacol. 1990 Mar;29(3):299-304. doi: 10.1111/j.1365-2125.1990.tb03639.x.
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