Yamane M, Abe A, Yanagisawa I
J Neurochem. 1984 Jun;42(6):1650-4. doi: 10.1111/j.1471-4159.1984.tb12755.x.
L-1- Methylheptyl -gamma- bromoacetoacetate was found to be a competitive inhibitor of the acetylcholinesterases (electric eel, Ki = 17.2 microM; rat brain, Ki = 32.6 microM) and of butyrylcholinesterase (horse serum, Ki = 1.2 microM). The L-isomer was a more effective inhibitor than the D-isomer. The bromine atom at the gamma-position of the acidic moiety, the specific length of the carbon chain constituting the secondary alcohol moiety, and the presence of the ketone radical at the acidic moiety of the ester were necessary for the anticholinesterase action. 1- Methylheptyl -gamma- bromoacetoacetate formed a complex with acetylcholinesterase or butyrylcholinesterase without hydrolysis of its own molecule.
发现L-1-甲基庚基-γ-溴代乙酰乙酸酯是乙酰胆碱酯酶（电鳗，Ki = 17.2微摩尔；大鼠脑，Ki = 32.6微摩尔）和丁酰胆碱酯酶（马血清，Ki = 1.2微摩尔）的竞争性抑制剂。L-异构体比D-异构体是更有效的抑制剂。酸性部分γ位的溴原子、构成仲醇部分的碳链的特定长度以及酯的酸性部分酮基的存在对于抗胆碱酯酶作用是必需的。1-甲基庚基-γ-溴代乙酰乙酸酯与乙酰胆碱酯酶或丁酰胆碱酯酶形成复合物，而其自身分子不发生水解。
