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血液和血浆中双硫仑的迅速减少。

The rapid reduction of disulfiram in blood and plasma.

作者信息

Cobby J, Mayersohn M, Selliah S

出版信息

J Pharmacol Exp Ther. 1977 Sep;202(3):724-31.

PMID:197231
Abstract

A gas chromatographic assay procedure was developed to quantitate the reduction product of disulfiram, diethyldithiocarbamate (DDC), in blood and plasma. The procedure involved the in situ methylation of DDC prior to the extraction and chromatography of the methyl ester. The minimal sensitivity achieved was 0.2 microgram/ml from 1 ml of blood or plasma. The coefficient of variation about any concentration was 10.5%. Calibration curves having a reproducible nonlinear form were prepared up to 9 microgram/ml. The assay procedure was used to evaluate the stability of disulfiram and DDC in blood. Disulfiram was rapidly and quantitatively reduced to DDC within 4 minutes. The DDC thus formed decomposed in human and dog blood with half-lives of 70 and 100 minutes, respectively. The implications of these findings are discussed with respect to the chemical form of disulfiram responsible for the ethanol-sensitizing effect.

摘要

已开发出一种气相色谱分析方法,用于定量测定血液和血浆中双硫仑的还原产物二乙基二硫代氨基甲酸盐(DDC)。该方法包括在提取和色谱分析甲酯之前对DDC进行原位甲基化。从1毫升血液或血浆中获得的最低灵敏度为0.2微克/毫升。任何浓度下的变异系数为10.5%。制备了浓度高达9微克/毫升的具有可重复非线性形式的校准曲线。该分析方法用于评估双硫仑和DDC在血液中的稳定性。双硫仑在4分钟内迅速定量还原为DDC。如此形成的DDC在人血和狗血中分解,半衰期分别为70分钟和100分钟。就负责乙醇增敏作用的双硫仑化学形式而言,讨论了这些发现的意义。

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The rapid reduction of disulfiram in blood and plasma.血液和血浆中双硫仑的迅速减少。
J Pharmacol Exp Ther. 1977 Sep;202(3):724-31.
2
Rapid degradation of disulfiram by serum albumin.双硫仑被血清白蛋白快速降解。
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Res Commun Chem Pathol Pharmacol. 1977 Jul;17(3):481-96.
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Diethyldithiocarbamate S-methylation: evidence for catalysis by human liver thiol methyltransferase and thiopurine methyltransferase.二乙基二硫代氨基甲酸盐的S-甲基化:人肝硫醇甲基转移酶和硫嘌呤甲基转移酶催化的证据。
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Rapid and sensitive on-line precolumn purification and high-performance liquid chromatographic assay for disulfiram and its metabolites.双硫仑及其代谢物的快速灵敏的在线柱前净化和高效液相色谱测定法
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Diethylthiocarbamic acid methyl ester. A potent inhibitor of aldehyde dehydrogenase found in rats treated with disulfiram or diethyldithiocarbamic acid methyl ester.二乙硫代氨基甲酸甲酯。在接受双硫仑或二乙二硫代氨基甲酸甲酯治疗的大鼠中发现的一种强效乙醛脱氢酶抑制剂。
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Quantitative analysis of disulfiram and its metabolites in human blood by gas-liquid chromatography.气液色谱法对人血液中双硫仑及其代谢物进行定量分析。
J Chromatogr. 1977 Mar 11;133(1):167-72. doi: 10.1016/s0021-9673(00)89217-1.

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