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剂量对非人灵长类动物中苯酚和1-萘酚结合模式的影响。

The influence of dose on the pattern of conjugation of phenol and 1-naphthol in non-human primates.

作者信息

Mehta R, Hirom P C, Millburn P

出版信息

Xenobiotica. 1978 Jul;8(7):445-52. doi: 10.3109/00498257809070029.

Abstract
  1. The pattern of conjugation of phenol and 1-naphthol was investigated in several primates; three Old World species (rhesus, cynomolgus, patas monkeys), two New World species (capuchin, tamarin), and two prosimians (bushbaby, tree shrew). 2. Following intra-muscular phenol or 1-naphthol (10 mg/kg), sulphation was the major conjugation in the Old World monkeys and prosimians, whereas glucuronidation predominated in the New World species. 3. In rhesus and cynomolgus monkeys, sulphation decreased as dose increased, but remained the major conjugation with both substrates at dose levels of 0.01 to 25 mg/kg. 4. In the capuchin, the conjugation pattern of phenol changed markedly as dose increased; at 0.01 and 1 mg/kg sulphation was the major conjugation, whereas at 10 and 25 mg/kg glucuronidation predominated. With 1-naphthol only small amounts of sulphate were excreted; glucuronic acid conjugation was the major metabolism at all four dose levels. 5. The importance of considering both substrate and dose when making inter-species comparisons, particularly with man, is discussed.
摘要
  1. 在几种灵长类动物中研究了苯酚和1-萘酚的结合模式;三种旧世界猴(恒河猴、食蟹猴、东非狒狒)、两种新世界猴(卷尾猴、绢毛猴)以及两种原猴亚目动物(婴猴、树鼩)。2. 肌肉注射苯酚或1-萘酚(10毫克/千克)后,硫酸化是旧世界猴和原猴亚目动物中的主要结合方式,而葡糖醛酸化在新世界猴中占主导。3. 在恒河猴和食蟹猴中,硫酸化随剂量增加而减少,但在0.01至25毫克/千克的剂量水平下,与两种底物的结合仍以硫酸化为主。4. 在卷尾猴中,苯酚的结合模式随剂量增加而显著变化;在0.01和1毫克/千克时硫酸化是主要结合方式,而在10和25毫克/千克时葡糖醛酸化占主导。对于1-萘酚,仅排泄少量硫酸盐;在所有四个剂量水平下,葡糖醛酸结合都是主要的代谢方式。5. 讨论了在进行种间比较时,特别是与人类进行比较时,同时考虑底物和剂量的重要性。

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