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人体内安替比林三种主要氧化代谢物的体内和体外生成速率比较。

Comparison of the in vivo and in vitro rates of formation of the three main oxidative metabolites of antipyrine in man.

作者信息

Boobis A R, Brodie M J, Kahn G C, Toverud E L, Blair I A, Murray S, Davies D S

出版信息

Br J Clin Pharmacol. 1981 Dec;12(6):771-7. doi: 10.1111/j.1365-2125.1981.tb01305.x.

DOI:10.1111/j.1365-2125.1981.tb01305.x
PMID:7340879
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1401933/
Abstract

1 The metabolism of antipyrine to its three main oxidative metabolites, 4-hydroxyantipyrine, 3-hydroxymethylantipyrine and norphenazone was investigated in vivo and in vitro in separate groups of subjects with normal hepatic function and in the same group of patients with suspected liver disease. 2 The rank order for the rate of formation of the three metabolites of antipyrine was similar in vivo and in vitro. 3 There was no significant correlation between the rates of formation of any pair of antipyrine metabolites either in vivo or in vitro. 4 Despite this there was a significant correlation between the in vivo and in vitro rates for formation of each of the three metabolites in the same group of patients. 5 It is concluded that determination of rates of formation of antipyrine metabolites from their excretion in urine provides an indication of the activity of the enzymes involved in their formation.

摘要
  1. 在肝功能正常的不同组受试者以及同一组疑似肝病患者中,对安替比林代谢为其三种主要氧化代谢物4 - 羟基安替比林、3 - 羟甲基安替比林和去甲非那宗的过程进行了体内和体外研究。2. 安替比林三种代谢物的生成速率在体内和体外的排序相似。3. 无论是在体内还是体外,任意一对安替比林代谢物的生成速率之间均无显著相关性。4. 尽管如此,同一组患者体内和体外三种代谢物各自的生成速率之间存在显著相关性。5. 得出结论,通过尿液排泄情况测定安替比林代谢物的生成速率可反映参与其生成的酶的活性。

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1
Comparison of the in vivo and in vitro rates of formation of the three main oxidative metabolites of antipyrine in man.人体内安替比林三种主要氧化代谢物的体内和体外生成速率比较。
Br J Clin Pharmacol. 1981 Dec;12(6):771-7. doi: 10.1111/j.1365-2125.1981.tb01305.x.
2
Antipyrine as a probe for human oxidative drug metabolism: identification of the cytochrome P450 enzymes catalyzing 4-hydroxyantipyrine, 3-hydroxymethylantipyrine, and norantipyrine formation.安替比林作为人类氧化药物代谢的探针:催化4-羟基安替比林、3-羟甲基安替比林和去甲安替比林形成的细胞色素P450酶的鉴定。
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3
Differential effects of 3-methylcholanthrene and phenobarbitone treatment on the oxidative metabolism of antipyrine in vitro by microsomal fractions of rat liver.
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Differential induction of antipyrine metabolism by rifampicin.利福平对安替比林代谢的差异诱导作用。
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Pol J Pharmacol. 2001 Jan-Feb;53(1):11-9.
6
Sex difference in antipyrine 3-hydroxylation. An in vivo-in vitro correlation of antipyrine metabolism in two rat strains.安替比林3-羟基化的性别差异。两种大鼠品系中安替比林代谢的体内-体外相关性。
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The effect of age on the oxidative metabolism of antipyrine by uninduced microsomal fractions of rat liver.
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High-performance liquid chromatographic method for the determination of the three main oxidative and 3-carboxylic antipyrine metabolites in human urine.
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引用本文的文献

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Effect of tacrine hydrochloride on hepatic drug metabolism.盐酸他克林对肝脏药物代谢的影响。
Eur J Drug Metab Pharmacokinet. 1999 Jan-Mar;24(1):91-6. doi: 10.1007/BF03190016.
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The relationship between phenazone (antipyrine) metabolite formation and theophylline metabolism in healthy and frail elderly women.健康及体弱老年女性中保泰松(安替比林)代谢产物形成与茶碱代谢之间的关系。
Clin Pharmacokinet. 1993 Aug;25(2):136-44. doi: 10.2165/00003088-199325020-00006.
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The acetylation phenotype: does it contribute to the non-linearity of the metabolite pharmacokinetics of metamizol?乙酰化表型:它是否导致了安乃近代谢物药代动力学的非线性?
Eur J Clin Pharmacol. 1995;48(1):79-80. doi: 10.1007/BF00202178.
4
Assay and characterisation of debrisoquine 4-hydroxylase activity of microsomal fractions of human liver.人肝脏微粒体组分中异喹胍4-羟化酶活性的测定与表征
Br J Clin Pharmacol. 1982 May;13(5):637-45. doi: 10.1111/j.1365-2125.1982.tb01430.x.
5
Antipyrine metabolism in relation to polymorphic oxidations of sparteine and debrisoquine.安替比林代谢与司巴丁和异喹胍多态性氧化的关系。
Br J Clin Pharmacol. 1983 Mar;15(3):317-21. doi: 10.1111/j.1365-2125.1983.tb01505.x.
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Tolbutamide as a model drug for the study of enzyme induction and enzyme inhibition in the rat.甲苯磺丁脲作为大鼠体内酶诱导和酶抑制研究的模型药物。
Br J Pharmacol. 1984 Mar;81(3):557-62. doi: 10.1111/j.1476-5381.1984.tb10109.x.
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Effect of chloroquine and primaquine on antipyrine metabolism.氯喹和伯氨喹对安替比林代谢的影响。
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Clin Pharmacokinet. 1983 Sep-Oct;8(5):371-7. doi: 10.2165/00003088-198308050-00001.
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Antipyrine clearance in patients with Gilbert's syndrome.吉尔伯特综合征患者的安替比林清除率
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Influence of rifampicin treatment on antipyrine clearance and metabolite formation in patients with tuberculosis.利福平治疗对肺结核患者安替比林清除率及代谢物形成的影响。
Br J Clin Pharmacol. 1984 Nov;18(5):701-6. doi: 10.1111/j.1365-2125.1984.tb02532.x.

本文引用的文献

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Protein measurement with the Folin phenol reagent.使用福林酚试剂进行蛋白质测定。
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An improved combined gas chromatographic mass spectrometric assay for the estimation of norphenazone in urine.一种用于测定尿液中去甲非那宗的改进型气相色谱-质谱联用分析法。
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Antipyrine as an in vitro probe of mixed function oxidase activity [proceeding].安替比林作为混合功能氧化酶活性的体外探针[会议论文]
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Correlations between cytochrome P-450 and oxidative metabolism of benzo[a]pyrene and 7-ethoxycoumarin in human liver in vitro and antipyrine elimination in vivo.体外人肝脏中细胞色素P-450与苯并[a]芘和7-乙氧基香豆素氧化代谢及体内安替比林消除之间的相关性。
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Genetic control of drug levels in man: antipyrine.人体药物水平的遗传控制:安替比林
Science. 1968 Jul 5;161(3836):72-3. doi: 10.1126/science.161.3836.72.
7
Genetic control of the phenobarbital-induced shortening of plasma antipyrine half-lives in man.苯巴比妥诱导人体血浆安替比林半衰期缩短的遗传控制。
J Clin Invest. 1969 Dec;48(12):2202-9. doi: 10.1172/JCI106186.
8
Correlation of the plasma elimination of antipyrine and the appearance of 4-hydroxy antipyrine in the urine of man.人体尿液中安替比林的血浆消除与4-羟基安替比林出现的相关性。
Biochem Pharmacol. 1974 Jan 15;23(2):197-201. doi: 10.1016/0006-2952(74)90410-9.
9
Comparison of plasma levels of antipyrine, tolbutamide, and warfarin after oral and intravenous administration.口服和静脉注射后安替比林、甲苯磺丁脲和华法林的血浆水平比较。
Clin Pharmacol Ther. 1974 Dec;16(6):1059-65. doi: 10.1002/cpt19741661059.
10
The effect of spironolactone on antipyrine metabolism in man.螺内酯对人体安替比林代谢的影响。
Pharmacology. 1973;10(6):338-44. doi: 10.1159/000136455.