李桦, 阮金秀, 汤炳生, 武力民, 贾敬山. 催醒安在大鼠尿内代谢产物的研究J. 药学学报, 1989, 24(4): 246-250.
引用本文: 李桦, 阮金秀, 汤炳生, 武力民, 贾敬山. 催醒安在大鼠尿内代谢产物的研究J. 药学学报, 1989, 24(4): 246-250.
H Li, JX Ruan, BS Tang, LM Wu , JS Jia, . STUDY ON THE METABOLITES OF CUI-XING-AN IN RAT URINEJ. Acta Pharmaceutica Sinica, 1989, 24(4): 246-250.
Citation: H Li, JX Ruan, BS Tang, LM Wu , JS Jia, . STUDY ON THE METABOLITES OF CUI-XING-AN IN RAT URINEJ. Acta Pharmaceutica Sinica, 1989, 24(4): 246-250.

催醒安在大鼠尿内代谢产物的研究

STUDY ON THE METABOLITES OF CUI-XING-AN IN RAT URINE

  • 摘要: 催醒安是一种新的中枢性抗胆碱酯酶药。给大鼠灌胃后,用HPLC分离纯化尿提取液中的代谢产物,得到四个组分。经MS鉴定分别为原形药物,N-羟甲基,N-甲基氨基甲酸-间-(2-二甲氨基)乙氧基苯酯(简称羟基化催醒安),N-甲基氨基甲酸-间-(2-二甲氨基)乙氧基苯酯(去甲基催醒安)及间-(2-二甲氨基)乙氧基苯酚(催醒安水解物)。原药及产物对电鳐乙酰胆碱酯酶抑制率的实验表明,去甲基催醒安抑酶活性与原药相近,羟基化催醒安活性比原药低,水解物无抑酶活性。

     

    Abstract: m-(2-Dimethylamino) ethoxy phenyl-N, N-dimethyl carbamate (Cui-Xing An) is a new central anticholinesterase drug. After oral administration of Cui-Xing-An to rats, four components were isolated and purified from urine extract by HPLC, They were identified by MS to be the parent drug, m-2-dimethylamino) ethoxy phenyl-N-hydroxymethyl-N-methyl carbamate (hydroxylated Cui-Xing-An), m-(2—dimethylamino) ethoxy phenyl-N-methyl carbamate (N-demethylated Cui-Xing-An) and m-(2-dimethylamino) ethoxy phenol (hydroly sate).Experiment on Torpediniforms Nacline timilei AchE inhibitory rate showed that the N-demethyl Cui-Xing-An had the same anticholinesterase activity as the parent drug. The hydroxylated Cui-Xing-An exhibited lower activity, and the hydrolysate was inactive.

     

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