论文部分内容阅读
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。
Awake Ann is a new central anticholinesterase drugs. After intragastric administration to rats, the metabolites in the urine extract were separated and purified by HPLC to obtain four fractions. MS were identified as the prototype drugs, N-methylol, N-methyl carbamic acid - [m- (2-dimethylamino)] ethoxy phenyl ester Carbamic acid- [meta- (2-dimethylamino) ethoxy] phenyl ester (desmethyl reminder) and meta- (2-dimethylamino) ethoxyphenol (reminder amphetamine). The former drug and the product of the electric 鳐 acetylcholinesterase inhibition rate experiments showed that the activity of desmethylammonium was similar to the original drug reminder activity of hydroxylation reminder safety than the original drug, hydrolyzate no inhibitory activity.