Murray S, Boobis A R, Frank H, Baillie T A, Davies D S
Naunyn Schmiedebergs Arch Pharmacol. 1980 Oct;314(1):89-96. doi: 10.1007/BF00498435.
3-Methoxy-4-hydroxyphenylethylene glycol (MHPG) labelled with six deuterium atoms ([2H6]MHPG) was infused into two female greyhound dogs. Plasma and urine were analyzed for endogenous MHPG and [2H6]MHPG and their conjugates by the technique of selected ion monitoring gas chromatography-mass spectrometry. This analysis showed that the major forms of MHPG and [2H6]MHPG in the plasma and urine of the greyhounds were the sulphate conjugates. However, the plasma concentration of [2H6]MHPG sulphate increased continuously during the infusion period and the renal clearance of this compound was found to be much less than that of the endogenous sulphate. The explanation that his was due either to saturation of a renal transport mechanism or to a deuterium isotope effect was eliminated. Stereochemical analysis showed that, while the [2H6]MHPG used for infusion was a racemic mixture of two stereoisomers, much more of the nature(-)stereoisomer of [2H6]MHPG sulphate was excreted in the dog urine. It was also shown that both the (+) and (-)stereoisomers of [2H6]MHPG sulphate were sulphoconjugated at the 4-position of the aromatic ring.
将标记有六个氘原子的3-甲氧基-4-羟基苯乙二醇（[2H6]MHPG）注入两只雌性灵缇犬体内。采用选择离子监测气相色谱-质谱技术分析血浆和尿液中的内源性MHPG、[2H6]MHPG及其结合物。该分析表明，灵缇犬血浆和尿液中MHPG和[2H6]MHPG的主要形式是硫酸结合物。然而，在输注期间，[2H6]MHPG硫酸盐的血浆浓度持续升高，且发现该化合物的肾清除率远低于内源性硫酸盐的肾清除率。肾转运机制饱和或氘同位素效应导致这种情况的解释被排除。立体化学分析表明，虽然用于输注的[2H6]MHPG是两种立体异构体的外消旋混合物，但[2H6]MHPG硫酸盐的天然（-）立体异构体更多地排泄到犬尿中。还表明，[2H6]MHPG硫酸盐的（+）和（-）立体异构体均在芳环的4位发生硫酸结合。
