大鼠肝脏在体内进行药物硫酸结合反应时血液中无机硫酸盐的可用性。（35S）硫酸盐掺入哈尔莫硫酸盐。
The availability of inorganic sulphate in blood for sulphate conjugation of drugs in rat liver in vivo. (35S)Sulphate incorporation into harmol sulphate.
作者信息
Mulder G J, Scholtens E
出版信息
Biochem J. 1978 May 15;172(2):247-51. doi: 10.1042/bj1720247.
Abstract
- When Na235SO4 is injected intravenously in rats, it is immediately available for sulphate conjugation of the phenolic drug harmol (7-hydroxyl-1-methyl-9H-pyrido[3,4-b]indole) in the liver. This was established by following the time course of the biliary excretion of the sulphate conjugate of harmol, and the incorporation of [35S]sulphate into harmol sulphate. 2. During the 10min immediately after injection of Na235SO4 re-distribution of [35S]sulphate took place, which resulted in a rapid initial decrease in the plasma concentration of [35S]sulphate; a concomitant decrease in the amount of [35S]sulphate incorporated into harmol sulphate was observed, indicating that the co-substrate of sulphation, adenosine 3'-phosphate 5'-sulphatophosphate, equilibrates rapidly with [35S]sulphate in plasma. 3. The results suggest that the pool size of adenosine 3'-phosphate 5'-sulphatophosphate is very small; therefore the specific radioactivity of [35S]sulphate in plasma determines the specific radioactivity incorporated into sulphate esters at any time.
摘要
- 当将Na₂³⁵SO₄静脉注射到大鼠体内时，它可立即用于肝脏中酚类药物哈尔醇（7-羟基-1-甲基-9H-吡啶并[3,4-b]吲哚）的硫酸结合反应。这是通过追踪哈尔醇硫酸结合物的胆汁排泄时间进程以及[³⁵S]硫酸掺入哈尔醇硫酸盐的情况来确定的。2. 在注射Na₂³⁵SO₄后的10分钟内，发生了[³⁵S]硫酸的重新分布，这导致血浆中[³⁵S]硫酸的浓度迅速初始下降；观察到掺入哈尔醇硫酸盐中的[³⁵S]硫酸量也随之下降，这表明硫酸化的共底物3'-磷酸腺苷5'-磷酸硫酸酯与血浆中的[³⁵S]硫酸迅速达到平衡。3. 结果表明，3'-磷酸腺苷5'-磷酸硫酸酯的库大小非常小；因此，血浆中[³⁵S]硫酸的比放射性决定了在任何时候掺入硫酸酯中的比放射性。
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