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双硫仑及其代谢产物二乙硫代氨基甲酸甲酯的血浆蛋白结合情况。

Plasma protein binding of disulfiram and its metabolite diethylthiocarbamic acid methyl ester.

作者信息

Johansson B

机构信息

Department of Clinical Chemistry, General Hospital, Malmö, Sweden.

出版信息

J Pharm Pharmacol. 1990 Nov;42(11):806-7. doi: 10.1111/j.2042-7158.1990.tb07028.x.

DOI:10.1111/j.2042-7158.1990.tb07028.x
PMID:1982309
Abstract

The human plasma protein binding of disulfiram and its metabolite, diethylthiocarbamic acid methyl ester has been studied by an ultrafiltration technique. Both compounds were bound principally to albumin (mean 96.1 and 79.5%) over the ranges 200-800 and 345-2756 nM, respectively. The average number of binding sites was approximately 1 for both substances, whereas the average association constants were 7.1 x 10(4) and 6.1 x 10(3) M-1, respectively. Log P (octanol/water) was 2.81 for disulfiram and 1.85 for diethylthiocarbamic acid methyl ester.

摘要

采用超滤技术研究了双硫仑及其代谢产物二乙硫代氨基甲酸甲酯与人血浆蛋白的结合情况。在200 - 800 nM和345 - 2756 nM范围内,这两种化合物主要与白蛋白结合(平均分别为96.1%和79.5%)。两种物质的平均结合位点数约为1个,而平均缔合常数分别为7.1×10⁴ M⁻¹和6.1×10³ M⁻¹。双硫仑的Log P(正辛醇/水)为2.81,二乙硫代氨基甲酸甲酯的Log P为1.85。

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