通过来自不同物种的经强化的9000g肝脏上清液将芳烷基肟代谢氧化为硝基化合物。

Metabolic oxidation of aralkyl oximes to nitro compounds by fortified 9000g liver supernatants from various species.

作者信息

Beckett A H, Jones G R

出版信息

J Pharm Pharmacol. 1977 Jul;29(7):416-21. doi: 10.1111/j.2042-7158.1977.tb11356.x.

DOI:10.1111/j.2042-7158.1977.tb11356.x

PMID:19580

Abstract

Incubation of 'amphetamine oxime' (IIa, anti-benzyl methyl ketoxime) with fortified rabbit liver 9000 g supernatants gave the nitro compound (Ie) and the beta-hydroxylated oxime (IIc) in addition to the previously reported ketone (IIb) and alcohol (Ic) metabolites. Formation of the products was cofactor dependent. The nitro compound was also formed using mouse, hamster and guinea-pig 9000 g liver supernatants and to a minor extent by rat liver. The oximes of 2-phenethylamine (IIe) and norfenfluramine (IIg) were also metabolized to the corresponding nitro compounds, ketones and alcohols with rabbit 9000 g liver supernatants; however, no nitro compound (IIIb) was detected after the incubation of 'mexiletine oxime' (IVa). The metabolic products were identified and characterized by g.l.c., t.l.c. and g.l.c. linked mass spectrometry by comparison with synthetic materials.

摘要

将“苯丙胺肟”（IIa，反苄基甲基酮肟）与强化兔肝9000g上清液一起温育，除了先前报道的酮（IIb）和醇（Ic）代谢产物外，还得到了硝基化合物（Ie）和β-羟基化肟（IIc）。产物的形成依赖于辅因子。使用小鼠、仓鼠和豚鼠9000g肝上清液也能形成硝基化合物，大鼠肝形成的量较少。用兔9000g肝上清液温育2-苯乙胺肟（IIe）和去甲氟西汀肟（IIg）时，它们也会代谢为相应的硝基化合物、酮和醇；然而，“美西律肟”（IVa）温育后未检测到硝基化合物（IIIb）。通过气相色谱、薄层色谱以及气相色谱-质谱联用，并与合成材料进行比较，对代谢产物进行了鉴定和表征。