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3-取代吡啶在各种动物体内的代谢性N-氧化作用。

The metabolic N-oxidation of 3-substituted pyridines in various animal species in vivo.

作者信息

Gorrod J W, Damani L A

出版信息

Eur J Drug Metab Pharmacokinet. 1980;5(1):53-7. doi: 10.1007/BF03189445.

Abstract

The intraperitoneal administration of pyridine, 3-methylpyridine and 3-chloropyridine to mice, hamsters, rats, guinea-pigs, rabbits and ferrets, resulted in the urinary excretion of their N-oxides. Pyridine-N-oxide was found to be a quantitatively important metabolite of pyridine in all the species studied; the percentage of the dose excreted in the urine as pyridine-N-oxide ranged from 10% in rats to about 40% in mice and guinea-pigs. 3-Chloropyridine-N-oxide and 3-methylpyridine-N-oxide accounted for less than 7% of the administered dose of the parent base. The urinary excretion of pyridine-N-oxide was considerably greater in mice pretreated with phenobarbitone, compared to control mice, whereas 3-methylchloranthrene pretreatment had no appreciable effect on the excretion of pyridine-N-oxide.

摘要

给小鼠、仓鼠、大鼠、豚鼠、兔子和雪貂腹腔注射吡啶、3-甲基吡啶和3-氯吡啶后,它们的N-氧化物会随尿液排出。在所有研究的物种中,吡啶-N-氧化物都是吡啶的一种在数量上很重要的代谢产物;以吡啶-N-氧化物形式随尿液排出的剂量百分比在大鼠中为10%,在小鼠和豚鼠中约为40%。3-氯吡啶-N-氧化物和3-甲基吡啶-N-氧化物占母体碱给药剂量的比例不到7%。与对照小鼠相比,用苯巴比妥预处理的小鼠中吡啶-N-氧化物的尿液排泄量显著增加,而用3-甲基氯蒽预处理对吡啶-N-氧化物的排泄没有明显影响。

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