新型毒扁豆碱衍生物对乙酰胆碱酯酶的抑制作用。
Inhibition of acetylcholinesterase by new physostigmine derivatives.
作者信息
Marta M, Pomponi M
机构信息
Chemistry Institute, U.C.S.C. A. Gemelli, School of Medicine, Rome, Italy.
出版信息
Biomed Biochim Acta. 1988;47(3):285-8.
The kinetics of inhibition of acetylcholinesterase (AChE, EC 3.1.1.7) from electric eel by new physostigmine derivatives in which the methylcarbamic group has been substituted with monoalkylcarbamic, dialkylcarbamic and phenylcarbamic groups was studied. The new compounds are competitive inhibitors of AChE and show a lower anticholinesterase activity than physostigmine. The anticholinesterase activity, the bimolecular rate constant ki and the carbamylation constant k2 have been measured for some selected derivatives.
研究了新的毒扁豆碱衍生物对电鳗乙酰胆碱酯酶（AChE，EC 3.1.1.7）的抑制动力学，这些衍生物中的甲基氨基甲酸基团已被单烷基氨基甲酸、二烷基氨基甲酸和苯基氨基甲酸基团取代。新化合物是AChE的竞争性抑制剂，且抗胆碱酯酶活性低于毒扁豆碱。已对一些选定的衍生物测定了抗胆碱酯酶活性、双分子速率常数ki和氨甲酰化常数k2。
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