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除草剂异丙甲草胺(巴农)在大鼠和犬体内的代谢情况。

The fate of the herbicide flamprop-isopropyl (barnon) in rats and dogs.

作者信息

Hutson D H, Crayford J V, Hoadley E C

出版信息

Xenobiotica. 1977 May;7(5):279-300. doi: 10.3109/00498257709035786.

DOI:10.3109/00498257709035786
PMID:899038
Abstract
  1. [14C]Flamprop-isoppropyl (BARNON) administered orally to rats and dogs is excreted mostly via the faeces (90-5% and 76-3% in male and female rats respectively and 53% in dogs). Elimination was rapid from both species, and greater than 96% of the dose of 14C was excreted by rats 0-48 h after dosing. Distribution of 14C between urine and faeces was different in male and female rats, but the same for dogs of either sex. 2. The predominant metabolic pathway in both species was loss of the isopropyl group; the resulting carboxylic acid was excreted free and as the ester glucuronide. 3. Aromatic hydroxylation occurred at the para- and meta-positions of the N-benzoyl ring; the presence of a 3,4-dihydroxybenzoyl metabolite (but no dihydrodiol) suggests that arene oxide formation is involved. However, direct hydroxylation at position 3 cannot be precluded. Aromatic hydroxylation occurred with the following facility (0-48 h); male rat, 18%; female rat, 13%; dog (either sex), 2%. 4. Hydroxylation occurred readily in the isopropyl side chain yielding mostly a propan-1,2-diol ester in the dog. In the rat, this metabolite was mostly oxidized to yield a 2-lactyl ester.
摘要
  1. 给大鼠和狗口服[14C]丙酯杀草丹(BARNON)后,其主要通过粪便排出(雄性和雌性大鼠分别为90 - 5%和76 - 3%,狗为53%)。两种动物的排泄都很快,给药后0 - 48小时,大鼠排出的14C剂量超过96%。雄性和雌性大鼠尿液和粪便中14C的分布不同,但不同性别的狗相同。2. 两种动物的主要代谢途径都是异丙基的丢失;生成的羧酸以游离形式和酯葡萄糖醛酸苷的形式排出。3. 芳环羟基化发生在N - 苯甲酰环的对位和间位;3,4 - 二羟基苯甲酰代谢物(但没有二氢二醇)的存在表明涉及环氧芳烃的形成。然而,不能排除在3位的直接羟基化。芳环羟基化的发生率如下(0 - 48小时):雄性大鼠为18%;雌性大鼠为13%;狗(任何性别)为2%。4. 异丙基侧链很容易发生羟基化,在狗体内主要生成1,2 - 丙二醇酯。在大鼠体内,这种代谢物大多被氧化生成2 - 乳酰酯。

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