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7-甲氧基-2-硝基萘并[2,1-b]呋喃在大鼠和小鼠体内的处置情况。

Disposition in rats and mice of 7-methoxy-2-nitronaphtho[2,1-b]furan.

作者信息

Maurizis J C, Madelmont J C, Parry D, Meyniel G, Buisson J P, Royer R

出版信息

Xenobiotica. 1985 Feb;15(2):141-8. doi: 10.3109/00498258509045344.

Abstract

The disposition of 7-methoxy-2-nitronaphtho[2,1-b]furan (MNNF), labelled with 14C in the furan ring (label 1) and in the methoxy group (label 2) has been studied in rats and mice. After i.p. administration to rat (5 mg/kg), both labelled species were absorbed by the lymphatics; and after oral administration, through the intestinal lumen. Excretion of the furan ring (label 1) is mainly urinary (44% dose in 24 h); label 2 was mostly expired as 14CO2 (48% dose in 24 h), indicating considerable demethylation. No target organ was found for MNNF, except liver and kidney. For both labelled species given orally, radioactivity was bound to the intestinal wall. Preliminary metabolic studies, using t.l.c. and h.p.l.c., have shown the presence of an urinary metabolite, namely, the glucuronide of 7-hydroxy-2-nitronaphtho[2,1-b]furan (15-20% of the urinary radioactivity). The remaining radioactivity comprises basic compounds, that bind to a cationic resin, which might be formed by enzymic reduction of the nitro group.

摘要

对在呋喃环(标记1)和甲氧基(标记2)上用¹⁴C标记的7-甲氧基-2-硝基萘并[2,1-b]呋喃(MNNF)在大鼠和小鼠体内的处置情况进行了研究。给大鼠腹腔注射(5毫克/千克)后,两种标记物均通过淋巴管吸收;口服给药后,则通过肠腔吸收。呋喃环(标记1)的排泄主要通过尿液(24小时内排出剂量的44%);标记2大部分以¹⁴CO₂形式呼出(24小时内排出剂量的48%),表明发生了相当程度的去甲基化。除肝脏和肾脏外,未发现MNNF的靶器官。对于口服给予的两种标记物,放射性均与肠壁结合。使用薄层层析和高效液相色谱进行的初步代谢研究表明,尿液中存在一种代谢产物,即7-羟基-2-硝基萘并[2,1-b]呋喃的葡糖醛酸苷(占尿液放射性的15 - 20%)。其余放射性包括与阳离子树脂结合的碱性化合物,这些碱性化合物可能是由硝基的酶促还原形成的。

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