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大鼠体内六甲基三聚氰胺和五甲基三聚氰胺的排泄途径。

Routes of elimination of hexamethylmelamine and pentamethylmelamine in the rat.

作者信息

Colombo T, Broggini M, Gescher A, D'Incalci M

出版信息

Xenobiotica. 1982 May;12(5):315-21. doi: 10.3109/00498258209052471.

DOI:10.3109/00498258209052471
PMID:6814076
Abstract
  1. In the rat 40% of a dose of 25 mg/kg of hexamethylmelamine or pentamethylmelamine was excreted in the urine as metabolites, more than 95% of which were N2N4-dimethylmelamine and monomethylmelamine. 2. Biliary excretion of hexamethylmelamine or pentamethylmelamine and their N-demethylated metabolites accounted for less than 2% of the administered dose. Only 0 X 3% was excreted with the faeces, suggesting that there is intestinal reabsorption of a portion of the methylmelamines passing into the bile. 3. Conjugates of methylmelamines with glucuronic acid or sulphate were found only in minute quantities in the urine or bile of rats treated with hexamethylmelamine or pentamethylmelamine. However a conjugation product of pentamethylmelamine, of as yet unknown nature, is a major metabolite after pentamethylmelamine treatment.
摘要
  1. 在大鼠中,25毫克/千克剂量的六甲基三聚氰胺或五甲基三聚氰胺有40%以代谢物形式经尿液排出,其中超过95%是N2N4 - 二甲基三聚氰胺和单甲基三聚氰胺。2. 六甲基三聚氰胺或五甲基三聚氰胺及其N - 去甲基代谢物的胆汁排泄量占给药剂量的比例不到2%。只有0.3%随粪便排出,这表明进入胆汁的部分甲基三聚氰胺存在肠重吸收现象。3. 在经六甲基三聚氰胺或五甲基三聚氰胺处理的大鼠的尿液或胆汁中,仅发现极少量的甲基三聚氰胺与葡萄糖醛酸或硫酸盐的结合物。然而,五甲基三聚氰胺的一种性质尚不清楚的结合产物是五甲基三聚氰胺处理后的主要代谢物。

相似文献

1
Routes of elimination of hexamethylmelamine and pentamethylmelamine in the rat.大鼠体内六甲基三聚氰胺和五甲基三聚氰胺的排泄途径。
Xenobiotica. 1982 May;12(5):315-21. doi: 10.3109/00498258209052471.
2
Determination of pentamethylmelamine and hexamethylmelamine in plasma and urine by nitrogen-phosphorus gas-liquid chromatography.用氮磷气相色谱法测定血浆和尿液中的五甲基三聚氰胺和六甲基三聚氰胺。
J Chromatogr. 1979 Jun 1;174(1):245-9. doi: 10.1016/s0021-9673(00)87062-4.
3
Disposition and metabolism of pentamethylmelamine and hexamethylmelamine in rabbits and humans.
Cancer Res. 1979 Dec;39(12):5016-21.
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Pharmacology of pentamethylmelamine in humans.五甲基三聚氰胺在人体中的药理学。
Cancer Res. 1981 Feb;41(2):566-9.
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Prodrugs of hydroxymethylpentamethylmelamine: a principal active metabolite of the antineoplastic agent hexamethylmelamine.羟甲基五甲基三聚氰胺的前药:抗肿瘤药六甲蜜胺的主要活性代谢物。
Drug Des Discov. 1994 Feb;11(2):135-47.
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Absorption and metabolism of hexamethylmelamine and pentamethylmelamine in rat everted perfused gut segments: correlation with in-vivo data.六甲基三聚氰胺和五甲基三聚氰胺在大鼠外翻灌注肠段中的吸收与代谢:与体内数据的相关性
J Pharm Pharmacol. 1985 Sep;37(9):629-36. doi: 10.1111/j.2042-7158.1985.tb05099.x.
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Rapid formation of N-hydroxymethylpentamethylmelamine by mitochondria from rat small intestinal epithelium.大鼠小肠上皮线粒体快速形成N-羟甲基五甲基三聚氰胺。
Life Sci. 1983 Nov 21;33(21):2113-9. doi: 10.1016/0024-3205(83)90335-1.
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Phase I and pharmacological studies of pentamethylmelamine administered by 24-hour intravenous infusion.
Cancer Res. 1981 Apr;41(4):1402-6.
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Metabolic activation of hexamethylmelamine and pentamethylmelamine by liver microsomal preparations.肝微粒体制剂对六甲蜜胺和五甲蜜胺的代谢激活作用。
Life Sci. 1981 Oct 12;29(15):1591-8. doi: 10.1016/0024-3205(81)90261-7.
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Phase I trial of pentamethylmelamine.
Cancer Treat Rep. 1982 May;66(5):1227-8.

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